TTD_Target_ID Target_Name TTD_Drug_ID Drug_Name Drug_Highest_Status Drug_PubchemID Molecular_Formula Molecular_Weight Canonical_SMILES Activity Binder_Type T63966 Vascular endothelial growth factor receptor 1 D0M0XB Saracatinib Phase 2 10302451 C27H32ClN5O5 542 CN1CCN(CC1)CCOC2=CC3=C(C(=C2)OC4CCOCC4)C(=NC=N3)NC5=C(C=CC6=C5OCO6)Cl IC50 ~ 100000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 B0CPW1 1-((5-(6-((4-Methylpiperazin-1-yl)methyl)-1,4-dihydroindeno[1,2-c]pyrazol-3-yl)thiophen-2-yl)methyl)-3-(2-(trifluoromethyl)phenyl)urea Investigative 44414847 C29H29F3N6OS 566.6 CN1CCN(CC1)CC2=CC3=C(C=C2)C4=NNC(=C4C3)C5=CC=C(S5)CNC(=O)NC6=CC=CC=C6C(F)(F)F IC50 ~ 50000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 B0K6WY (3R,6S,9S,14S,17S,23S,26S)-9-[[(2S)-2-Acetamido-4-methylsulfanylbutanoyl]amino]-3-(4-aminobutyl)-N-[(2S,3S)-1-amino-3-methyl-1-oxopentan-2-yl]-17-(3-amino-3-oxopropyl)-6-[(2S)-butan-2-yl]-23-(1H-imidazol-5-ylmethyl)-2,5,8,16,19,22,25-heptaoxo-1,4,7,15,18,21,24-heptazabicyclo[24.3.0]nonacosane-14-carboxamide Investigative 53320001 C51H85N15O12S 1132.4 CC[C@H](C)[C@H]1C(=O)N[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CCCC[C@@H](C(=O)N1)NC(=O)[C@H](CCSC)NC(=O)C)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N)CCC(=O)N)CC3=CN=CN3)CCCCN IC50 = 91600 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 B0X2YZ 3-[(3S,6S,9S,12R,17R,20S,23S,26S,29S,32S,35S,38S)-12-Amino-9-(3-amino-3-oxopropyl)-20,29-bis[(2S)-butan-2-yl]-26,32-bis(2-carboxyethyl)-35-(carboxymethyl)-17-[[(2S)-1,6-diamino-1-oxohexan-2-yl]carbamoyl]-3,23-bis[(4-hydroxyphenyl)methyl]-2,5,8,11,19,22,25,28,31,34,37-undecaoxo-14,15-dithia-1,4,7,10,18,21,24,27,30,33,36-undecazabicyclo[36.3.0]hentetracontan-6-yl]propanoic acid Investigative 137635974 C71H104N16O24S2 1629.8 CC[C@H](C)[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CSSC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CCC(=O)O)CC(=O)O)CC3=CC=C(C=C3)O)CCC(=O)O)CCC(=O)N)N)C(=O)N[C@@H](CCCCN)C(=O)N)[C@@H](C)CC)CC4=CC=C(C=C4)O)CCC(=O)O IC50 = 50400 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 B14NHR N-(1-Phenylethyl)-4-(2-(6-phenylimidazo[2,1-b]thiazol-5-yl)vinyl)pyrimidin-2-amine Investigative 44586767 C25H21N5S 423.5 CC(C1=CC=CC=C1)NC2=NC=CC(=N2)/C=C/C3=C(N=C4N3C=CS4)C5=CC=CC=C5 IC50 = 84000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 B18DEM c[YYDEALEE]-NH2 Investigative 46831064 C46H61N9O17 1012 C[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CCC(=O)O)CC(=O)O)CC2=CC=C(C=C2)O)CC3=CC=C(C=C3)O)C(=O)N)CCC(=O)O)CC(C)C IC50 = 101000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 B18EWX (E/Z)-N-(4-(2-(6-Phenylimidazo[2,1-b]thiazol-5-yl)vinyl)pyrimidin-2-yl)acetamide Investigative 44586769 C19H15N5OS 361.4 CC(=O)NC1=NC=CC(=N1)/C=C/C2=C(N=C3N2C=CS3)C4=CC=CC=C4 IC50 = 100000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 B18RWA N-(5-Chloro-1,3-benzodioxol-4-yl)-6-methoxy-7-(3-morpholin-4-ylpropoxy)quinazolin-4-amine Investigative 5330188 C23H25ClN4O5 472.9 COC1=C(C=C2C(=C1)C(=NC=N2)NC3=C(C=CC4=C3OCO4)Cl)OCCCN5CCOCC5 IC50 ~ 100000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 B1C2UF Cyclo[FYDEPLEbtA]-NH2 Investigative 44444796 C49H63N13O16 1090.1 CC(C)C[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CC2=CN(N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N3CCC[C@H]3C(=O)NC(=O)N1)CCC(=O)O)CC(=O)O)CC4=CC=C(C=C4)O)CC5=CC=CC=C5)N=N2)C(=O)N)CCC(=O)O IC50 = 93000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 B1JZB8 N-[4-(3-Ethynylanilino)-6-(2-pyridin-2-ylethyl)-7H-pyrrolo[2,3-d]pyrimidin-2-yl]-2,2-dimethylpropanamide Investigative 71525285 C26H26N6O 438.5 CC(C)(C)C(=O)NC1=NC2=C(C=C(N2)CCC3=CC=CC=N3)C(=N1)NC4=CC=CC(=C4)C#C IC50 = 156300 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 B1M2TH N4-(3-Bromophenyl)-6-(3,4,5-trimethoxybenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine Investigative 3008965 C22H22BrN5O3 484.3 COC1=CC(=CC(=C1OC)OC)CC2=CC3=C(N2)N=C(N=C3NC4=CC(=CC=C4)Br)N IC50 ~ 50000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 B2CL6O N-(3-Bromophenyl)-6-(2,4-dichlorobenzyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine Investigative 46887111 C19H13BrCl2N4 448.1 C1=CC(=CC(=C1)Br)NC2=NC=NC3=C2C=C(N3)CC4=C(C=C(C=C4)Cl)Cl IC50 = 150900 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 B2ZJ3E 4-(2-(1-Methyl-4-phenyl-1H-imidazol-5-yl)cyclopropyl)pyrimidin-2-amine Investigative 44586929 C17H17N5 291.35 CN1C=NC(=C1C2CC2C3=NC(=NC=C3)N)C4=CC=CC=C4 IC50 ~ 100000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 B3A9GH (3r)-1-{2-[4-(4-Acetylphenyl)piperazin-1-Yl]-2-Oxoethyl}-N-(3-Chloro-4-Hydroxyphenyl)pyrrolidine-3-Carboxamide Investigative 58985201 C25H29ClN4O4 485 CC(=O)C1=CC=C(C=C1)N2CCN(CC2)C(=O)CN3CC[C@H](C3)C(=O)NC4=CC(=C(C=C4)O)Cl IC50 ~ 50000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 B3D4VI 6-[(2,4-Dichlorophenyl)methyl]-4-N-(3-fluorophenyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine Investigative 46886971 C19H14Cl2FN5 402.2 C1=CC(=CC(=C1)F)NC2=NC(=NC3=C2C=C(N3)CC4=C(C=C(C=C4)Cl)Cl)N IC50 = 162900 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 B3HI9C (E/Z)-N-(4-(2-(6-Phenylimidazo[2,1-b]thiazol-5-yl)vinyl)pyrimidin-2-yl)pivalamide Investigative 44586770 C22H21N5OS 403.5 CC(C)(C)C(=O)NC1=NC=CC(=N1)/C=C/C2=C(N=C3N2C=CS3)C4=CC=CC=C4 IC50 = 96000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 B3MWL2 N4-(3-Bromophenyl)-6-(2,4-dichlorobenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine Investigative 3008956 C19H14BrCl2N5 463.2 C1=CC(=CC(=C1)Br)NC2=NC(=NC3=C2C=C(N3)CC4=C(C=C(C=C4)Cl)Cl)N IC50 ~ 50000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 B3QX6N 4-N-(3-Ethynylphenyl)-6-(2-pyridin-2-ylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine Investigative 71525247 C21H18N6 354.4 C#CC1=CC(=CC=C1)NC2=NC(=NC3=C2C=C(N3)CCC4=CC=CC=N4)N IC50 = 103100 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 B4AC8G 4-N-(3-Bromophenyl)-7-[(3,4,5-trimethoxyphenyl)methyl]pyrrolo[2,3-d]pyrimidine-2,4-diamine Investigative 57384106 C22H22BrN5O3 484.3 COC1=CC(=CC(=C1OC)OC)CN2C=CC3=C(N=C(N=C32)N)NC4=CC(=CC=C4)Br IC50 = 156500 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 B52FED N-(3-Ethynylphenyl)-6-(2-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine Investigative 46887298 C22H18N4 338.4 C#CC1=CC(=CC=C1)NC2=NC=NC3=C2C=C(N3)CCC4=CC=CC=C4 IC50 = 142300 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 B5P9HU 2-Amino-N-(1-methyl-4-phenyl-1H-imidazol-5-yl)pyrimidine-4-carboxamide Investigative 44586900 C15H14N6O 294.31 CN1C=NC(=C1NC(=O)C2=NC(=NC=C2)N)C3=CC=CC=C3 IC50 ~ 100000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 B5RM0K (4S,6R)-6-Bromo-18-hydroxy-16-methoxy-4-methyl-3-oxabicyclo[12.4.0]octadeca-1(14),15,17-triene-2,8-dione Investigative 53316977 C19H25BrO5 413.3 C[C@H]1C[C@H](CC(=O)CCCCCC2=C(C(=CC(=C2)OC)O)C(=O)O1)Br IC50 ~ 100000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 B5UOP1 4-N-(3-Bromophenyl)-7-[(4-chlorophenyl)methyl]pyrrolo[2,3-d]pyrimidine-2,4-diamine Investigative 57394880 C19H15BrClN5 428.7 C1=CC(=CC(=C1)Br)NC2=C3C=CN(C3=NC(=N2)N)CC4=CC=C(C=C4)Cl IC50 = 79900 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 B68NOA N-(3-Chloro-4-fluorophenyl)-6,7-dimethoxyquinazolin-4-amine Investigative 5329009 C16H13ClFN3O2 333.74 COC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=C(C=C3)F)Cl)OC IC50 ~ 100000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 B6FPS1 4-N-(3-Bromophenyl)-7-[(2-methylphenyl)methyl]pyrrolo[2,3-d]pyrimidine-2,4-diamine Investigative 57396646 C20H18BrN5 408.3 CC1=CC=CC=C1CN2C=CC3=C(N=C(N=C32)N)NC4=CC(=CC=C4)Br IC50 = 129300 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 B7XZN5 (E/Z)-4-(2-(3-Phenylthiophen-2-yl)vinyl)pyrimidin-2-amine Investigative 44586833 C16H13N3S 279.4 C1=CC=C(C=C1)C2=C(SC=C2)/C=C/C3=NC(=NC=C3)N IC50 ~ 100000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 B82GQV Cyclo[KYDEPLEbtA]-NH2 Investigative 44444803 C45H65N13O15 1028.099 CC(C)C[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CC2=CN(N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N3CCC[C@H]3C(=O)N1)CCC(=O)O)CC(=O)O)CC4=CC=C(C=C4)O)CCCCN)N=N2)C(=O)N)CCC(=O)O IC50 = 162000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 B8MF5X N-(3-Bromophenyl)-6-(2-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine Investigative 46887255 C20H17BrN4 393.3 C1=CC=C(C=C1)CCC2=CC3=C(N2)N=CN=C3NC4=CC(=CC=C4)Br IC50 = 129400 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 B8SJ4Q (E/Z)-N-Phenyl-4-(2-(6-phenylimidazo[2,1-b]thiazol-5-yl)vinyl)pyrimidin-2-amine Investigative 44586768 C23H17N5S 395.5 C1=CC=C(C=C1)C2=C(N3C=CSC3=N2)/C=C/C4=NC(=NC=C4)NC5=CC=CC=C5 IC50 ~ 100000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 B8T1KO 7-Benzyl-4-N-(3-bromophenyl)pyrrolo[2,3-d]pyrimidine-2,4-diamine Investigative 57394879 C19H16BrN5 394.3 C1=CC=C(C=C1)CN2C=CC3=C(N=C(N=C32)N)NC4=CC(=CC=C4)Br IC50 = 99300 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 B92RNM 4-{(E)-2-[4-Phenyl-1-(2-pyrrolidin-1-ylethyl)-1H-imidazol-5-yl]vinyl}pyrimidin-2-amine Investigative 44586896 C21H24N6 360.5 C1CCN(C1)CCN2C=NC(=C2/C=C/C3=NC(=NC=C3)N)C4=CC=CC=C4 IC50 ~ 100000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 B98XBU 4-N-(3-Methyl-5-phenylimidazol-4-yl)pyrimidine-2,4-diamine Investigative 44586898 C14H14N6 266.3 CN1C=NC(=C1NC2=NC(=NC=C2)N)C3=CC=CC=C3 IC50 ~ 100000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 B9IA6L N-(4-Chloro-2-fluorophenyl)-6-methoxy-7-(2-methoxyethoxy)cinnolin-4-amine Investigative 6326408 C18H17ClFN3O3 377.8 COCCOC1=C(C=C2C(=C1)N=NC=C2NC3=C(C=C(C=C3)Cl)F)OC IC50 = 63000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 B9N8WV N-(2-Aminopyrimidin-4-yl)-1-methyl-4-phenyl-1H-imidazole-5-carboxamide Investigative 44586899 C15H14N6O 294.31 CN1C=NC(=C1C(=O)NC2=NC(=NC=C2)N)C3=CC=CC=C3 IC50 ~ 100000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 B9Q4WV 4-N-(3-Bromophenyl)-6-(2-pyridin-2-ylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine Investigative 10047098 C19H17BrN6 409.3 C1=CC=NC(=C1)CCC2=CC3=C(N2)N=C(N=C3NC4=CC(=CC=C4)Br)N IC50 ~ 50000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BA21TR N-(5-Chloro-1,3-benzodioxol-4-yl)-6-methoxy-7-[(1-methylpiperidin-4-yl)methoxy]quinazolin-4-amine Investigative 5330196 C23H25ClN4O4 456.9 CN1CCC(CC1)COC2=C(C=C3C(=C2)N=CN=C3NC4=C(C=CC5=C4OCO5)Cl)OC IC50 ~ 100000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BAW04S 4-N-(3-Bromophenyl)-7-[(2,4-dichlorophenyl)methyl]pyrrolo[2,3-d]pyrimidine-2,4-diamine Investigative 57394786 C19H14BrCl2N5 463.2 C1=CC(=CC(=C1)Br)NC2=C3C=CN(C3=NC(=N2)N)CC4=C(C=C(C=C4)Cl)Cl IC50 = 138100 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BBWJ97 2-Benzyl-N4-(3-bromophenyl)-1H-indole-4,6-diamine Investigative 3008958 C19H16BrN5 394.3 C1=CC=C(C=C1)CC2=CC3=C(N2)N=C(N=C3NC4=CC(=CC=C4)Br)N IC50 ~ 50000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BDL8X6 1-(2-Chlorophenyl)-3-((5-(6-((4-methylpiperazin-1-yl)methyl)-1,4-dihydroindeno[1,2-c]pyrazol-3-yl)thiophen-2-yl)methyl)urea Investigative 44414659 C28H29ClN6OS 533.1 CN1CCN(CC1)CC2=CC3=C(C=C2)C4=NNC(=C4C3)C5=CC=C(S5)CNC(=O)NC6=CC=CC=C6Cl IC50 ~ 50000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BE9C0U N4-(2-Isopropylphenyl)-6-(2,4-dichlorobenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine Investigative 46887039 C22H21Cl2N5 426.3 CC(C)C1=CC=CC=C1NC2=NC(=NC3=C2C=C(N3)CC4=C(C=C(C=C4)Cl)Cl)N IC50 = 163100 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BEC69I N4-(3-Bromophenyl)-6-(2-methylbenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine Investigative 3008961 C20H18BrN5 408.3 CC1=CC=CC=C1CC2=CC3=C(N2)N=C(N=C3NC4=CC(=CC=C4)Br)N IC50 ~ 50000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BFB3R5 N-Methyl-4-[(E)-2-(6-phenylimidazo[2,1-b][1,3]thiazol-5-yl)vinyl]pyrimidin-2-amine Investigative 44587326 C18H15N5S 333.4 CNC1=NC=CC(=N1)/C=C/C2=C(N=C3N2C=CS3)C4=CC=CC=C4 IC50 = 77000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BFOR28 N-[4-[4-Fluoro-3-(trifluoromethyl)anilino]-6-(2-pyridin-2-ylethyl)-7H-pyrrolo[2,3-d]pyrimidin-2-yl]-2,2-dimethylpropanamide Investigative 71525287 C25H24F4N6O 500.5 CC(C)(C)C(=O)NC1=NC2=C(C=C(N2)CCC3=CC=CC=N3)C(=N1)NC4=CC(=C(C=C4)F)C(F)(F)F IC50 = 189600 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BH1MY2 Anilinoquinazoline deriv. 31 Investigative 5329029 C18H16ClFN4O3 390.8 COCC(=O)NC1=C(C=C2C(=C1)N=CN=C2NC3=C(C=C(C=C3)Cl)F)OC IC50 ~ 100000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BHP35J Geranin B Investigative 44566353 C30H24O11 560.5 C1[C@@H]([C@H](OC2=C1C(=CC3=C2[C@@H]4[C@H]([C@](O3)(OC5=CC(=CC(=C45)O)O)C6=CC(=C(C=C6)O)O)O)O)C7=CC=C(C=C7)O)O IC50 = 65000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BHP90Y (2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-Acetamido-4-methylsulfanylbutanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-methylpentanoyl]amino]-6-aminohexanoyl]pyrrolidine-2-carbonyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-5-amino-5-oxopentanoyl]amino]acetyl]amino]-N-[(2S)-1-[[(2S,3S)-1-amino-3-methyl-1-oxopentan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]pentanediamide Investigative 53318682 C60H100N22O14S 1385.6 CC[C@H](C)[C@@H](C(=O)N)NC(=O)[C@H](CC1=CN=CN1)NC(=O)[C@H](CCC(=O)N)NC(=O)CNC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](CC2=CN=CN2)NC(=O)[C@@H]3CCCN3C(=O)[C@H](CCCCN)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CCSC)NC(=O)C IC50 = 102700 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BIB1E3 4-(2-(1-Methyl-4-phenyl-1H-imidazol-5-ylamino)ethyl)pyrimidin-2-amine Investigative 44586928 C16H18N6 294.35 CN1C=NC(=C1NCCC2=NC(=NC=C2)N)C3=CC=CC=C3 IC50 ~ 100000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BJ9T1E 3-[(3S,6S,9S,12R,17R,20S,23S,26S,29S,32S,35S,38S)-12-Amino-17-[[(2S)-1-amino-3-hydroxy-1-oxopropan-2-yl]carbamoyl]-26,32-bis(2-carboxyethyl)-9,35-bis(hydroxymethyl)-3-[(4-hydroxyphenyl)methyl]-23-(1H-imidazol-5-ylmethyl)-20-(2-methylsulfanylethyl)-2,5,8,11,19,22,25,28,31,34,37-undecaoxo-29-propan-2-yl-14,15-dithia-1,4,7,10,18,21,24,27,30,33,36-undecazabicyclo[36.3.0]hentetracontan-6-yl]propanoic acid Investigative 137650005 C60H88N16O23S3 1497.6 CC(C)[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CSSC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CCC(=O)O)CO)CC3=CC=C(C=C3)O)CCC(=O)O)CO)N)C(=O)N[C@@H](CO)C(=O)N)CCSC)CC4=CN=CN4)CCC(=O)O IC50 = 56000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BJR71S (4S)-5-[[(2S)-1-Amino-1-oxopent-4-yn-2-yl]amino]-4-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-azido-2-phenylacetyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-carboxypropanoyl]amino]-4-carboxybutanoyl]pyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]-5-oxopentanoic acid Investigative 73345638 C47H59N11O15 1018 CC(C)C[C@@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC#C)C(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC2=CC=C(C=C2)O)NC(=O)[C@H](C3=CC=CC=C3)N=[N+]=[N-] IC50 = 96000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BK2GQ1 N-Benzyl-N-methyl-4-(phenylsulfamoyl)benzamide Investigative 27666048 C21H20N2O3S 380.5 CN(CC1=CC=CC=C1)C(=O)C2=CC=C(C=C2)S(=O)(=O)NC3=CC=CC=C3 IC50 ~ 100000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BK72AZ (E/Z)-4-(2-(2-Phenylthiophen-3-yl)vinyl)pyrimidin-2-amine Investigative 44586868 C16H13N3S 279.4 C1=CC=C(C=C1)C2=C(C=CS2)/C=C/C3=NC(=NC=C3)N IC50 ~ 100000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BKBE69 (2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-Acetamido-4-methylsulfanylbutanoyl]amino]pent-4-enoyl]amino]-3-methylpentanoyl]amino]-6-aminohexanoyl]pyrrolidine-2-carbonyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-5-amino-5-oxopentanoyl]amino]acetyl]amino]-N-[(2S)-1-[[(2S,3S)-1-amino-3-methyl-1-oxopentan-2-yl]amino]-1-oxopent-4-en-2-yl]pentanediamide Investigative 53322631 C58H95N17O14S 1286.5 CC[C@H](C)[C@@H](C(=O)N)NC(=O)[C@H](CC=C)NC(=O)[C@H](CCC(=O)N)NC(=O)CNC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](CC1=CN=CN1)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCCN)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CC=C)NC(=O)[C@H](CCSC)NC(=O)C IC50 = 61200 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BLGH87 N-(5-Chloro-1,3-benzodioxol-4-yl)-6-methoxy-7-(3-piperidin-1-ylpropoxy)quinazolin-4-amine Investigative 5330197 C24H27ClN4O4 470.9 COC1=C(C=C2C(=C1)C(=NC=N2)NC3=C(C=CC4=C3OCO4)Cl)OCCCN5CCCCC5 IC50 ~ 100000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BLKE67 4-N-(3-Bromophenyl)-6-[(4-phenylphenyl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine Investigative 3008960 C25H20BrN5 470.4 C1=CC=C(C=C1)C2=CC=C(C=C2)CC3=CC4=C(N3)N=C(N=C4NC5=CC(=CC=C5)Br)N IC50 ~ 50000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BLZ42H 4-[(E)-2-(6-Methylimidazo[2,1-b][1,3]thiazol-5-yl)ethenyl]pyrimidin-2-amine Investigative 44587324 C12H11N5S 257.32 CC1=C(N2C=CSC2=N1)/C=C/C3=NC(=NC=C3)N IC50 ~ 100000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BMP16I Cyclo[GHQMFYYbtA]-NH2 Investigative 44444786 C51H63N15O11S 1094.2 CSCCC[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CC2=CN(NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CCC(=O)N)CC3=CN=CN3)N=N2)C(=O)N)CC4=CC=C(C=C4)O)CC5=CC=C(C=C5)O)CC6=CC=CC=C6 IC50 = 121000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BNJM48 2,2-Dimethyl-N-[6-(2-pyridin-2-ylethyl)-4-[3-(trifluoromethyl)anilino]-7H-pyrrolo[2,3-d]pyrimidin-2-yl]propanamide Investigative 71525286 C25H25F3N6O 482.5 CC(C)(C)C(=O)NC1=NC2=C(C=C(N2)CCC3=CC=CC=N3)C(=N1)NC4=CC=CC(=C4)C(F)(F)F IC50 = 129600 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BNV2R7 (4S,6Z)-18-Hydroxy-16-methoxy-4-methyl-3-oxabicyclo[12.4.0]octadeca-1(14),6,15,17-tetraene-2,8-dione Investigative 49842779 C19H24O5 332.4 C[C@H]1C/C=C\\C(=O)CCCCCC2=C(C(=CC(=C2)OC)O)C(=O)O1 IC50 ~ 100000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BO92CT N4-(4-Isopropylphenyl)-6-(2,4-dichlorobenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine Investigative 46887038 C22H21Cl2N5 426.3 CC(C)C1=CC=C(C=C1)NC2=NC(=NC3=C2C=C(N3)CC4=C(C=C(C=C4)Cl)Cl)N IC50 = 157000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BOE94S 5-[(4-Methylphenyl)thio]-9h-pyrimido[4,5-b]indole-2,4-diamine Investigative 25218207 C17H15N5S 321.4 CC1=CC=C(C=C1)SC2=CC=CC3=C2C4=C(N=C(N=C4N3)N)N IC50 = 160100 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BOHV12 4-N-(3-Bromo-4-fluorophenyl)-6-(2-pyridin-2-ylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine Investigative 71525245 C19H16BrFN6 427.3 C1=CC=NC(=C1)CCC2=CC3=C(N2)N=C(N=C3NC4=CC(=C(C=C4)F)Br)N IC50 = 93600 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BOKW86 2-[(E)-2-(6-Phenylimidazo[2,1-b][1,3]thiazol-5-yl)ethenyl]pyrimidin-4-amine Investigative 44586829 C17H13N5S 319.4 C1=CC=C(C=C1)C2=C(N3C=CSC3=N2)/C=C/C4=NC=CC(=N4)N IC50 ~ 100000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BP61CA (4S)-4-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-Amino-2-azidohexanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-carboxypropanoyl]amino]-4-carboxybutanoyl]pyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]-5-[[(2S)-1-amino-1-oxopent-4-yn-2-yl]amino]-5-oxopentanoic acid Investigative 73351741 C45H64N12O15 1013.1 CC(C)C[C@@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC#C)C(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC2=CC=C(C=C2)O)NC(=O)[C@H](CCCCN)N=[N+]=[N-] IC50 = 151000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BP7XF8 3-[(3S,6S,9S,12S,21S,24S,27S,30S,33S,36S,39S,42S)-12-Acetamido-9-(3-amino-3-oxopropyl)-24,33-bis[(2S)-butan-2-yl]-30,36-bis(2-carboxyethyl)-39-(carboxymethyl)-21-[[(2S)-1,6-diamino-1-oxohexan-2-yl]carbamoyl]-3,27-bis[(4-hydroxyphenyl)methyl]-2,5,8,11,18,23,26,29,32,35,38,41-dodecaoxo-1,4,7,10,17,22,25,28,31,34,37,40-dodecazabicyclo[40.3.0]pentatetracontan-6-yl]propanoic acid Investigative 137639956 C78H115N17O26 1706.8 CC[C@H](C)[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)NCCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CCC(=O)O)CC(=O)O)CC3=CC=C(C=C3)O)CCC(=O)O)CCC(=O)N)NC(=O)C)C(=O)N[C@@H](CCCCN)C(=O)N)[C@@H](C)CC)CC4=CC=C(C=C4)O)CCC(=O)O IC50 = 75100 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BPLH59 4-N-(3-Bromophenyl)-7-[(3,4-dichlorophenyl)methyl]pyrrolo[2,3-d]pyrimidine-2,4-diamine Investigative 57398331 C19H14BrCl2N5 463.2 C1=CC(=CC(=C1)Br)NC2=C3C=CN(C3=NC(=N2)N)CC4=CC(=C(C=C4)Cl)Cl IC50 = 118600 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BQ1AM8 (4S,6E,12E)-18-Hydroxy-16-methoxy-4-methyl-3-oxabicyclo[12.4.0]octadeca-1(14),6,12,15,17-pentaene-2,8-dione Investigative 49842666 C19H22O5 330.4 C[C@H]1C/C=C/C(=O)CCC/C=C/C2=C(C(=CC(=C2)OC)O)C(=O)O1 IC50 = 51000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BQ9Y5W 2-[9-(4-Amino-3-methoxyphenyl)-6-oxo-5,11-dihydrobenzo[b][1,4]benzodiazepin-3-yl]-N-(4-morpholin-4-ylphenyl)acetamide Investigative 44427518 C32H31N5O4 549.6 COC1=C(C=CC(=C1)C2=CC3=C(C=C2)C(=O)NC4=C(N3)C=CC(=C4)CC(=O)NC5=CC=C(C=C5)N6CCOCC6)N IC50 ~ 50000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BQH90J 4-N-(3-Bromophenyl)-7-(naphthalen-1-ylmethyl)pyrrolo[2,3-d]pyrimidine-2,4-diamine Investigative 57394787 C23H18BrN5 444.3 C1=CC=C2C(=C1)C=CC=C2CN3C=CC4=C(N=C(N=C43)N)NC5=CC(=CC=C5)Br IC50 = 150000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BR79GT 3-[(3S,6S,9S,12S,15R,20R,23S,26S,29S,32S,35S,38S,41S)-15-Amino-9-(3-amino-3-oxopropyl)-12-benzyl-23,32-bis[(2S)-butan-2-yl]-29,35-bis(2-carboxyethyl)-38-(carboxymethyl)-20-[[(2S)-1,6-diamino-1-oxohexan-2-yl]carbamoyl]-3,26-bis[(4-hydroxyphenyl)methyl]-2,5,8,11,14,22,25,28,31,34,37,40-dodecaoxo-17,18-dithia-1,4,7,10,13,21,24,27,30,33,36,39-dodecazabicyclo[39.3.0]tetratetracontan-6-yl]propanoic acid Investigative 137643789 C80H113N17O25S2 1777 CC[C@H](C)[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CSSC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CCC(=O)O)CC(=O)O)CC3=CC=C(C=C3)O)CCC(=O)O)CCC(=O)N)CC4=CC=CC=C4)N)C(=O)N[C@@H](CCCCN)C(=O)N)[C@@H](C)CC)CC5=CC=C(C=C5)O)CCC(=O)O IC50 = 157400 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BS74TN 4-[(E)-2-(2-Phenylimidazo[1,2-a]pyridin-3-yl)vinyl]pyrimidin-2-amine Investigative 44586834 C19H15N5 313.4 C1=CC=C(C=C1)C2=C(N3C=CC=CC3=N2)/C=C/C4=NC(=NC=C4)N IC50 = 79000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BS9TZ1 N-[4-Fluoro-3-(trifluoromethyl)phenyl]-6-(2-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine Investigative 46887348 C21H16F4N4 400.4 C1=CC=C(C=C1)CCC2=CC3=C(N2)N=CN=C3NC4=CC(=C(C=C4)F)C(F)(F)F IC50 = 164300 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BSC93W (2S)-2-[[2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-Acetamido-4-methylsulfanylbutanoyl]amino]pent-4-enoyl]amino]-3-methylpentanoyl]amino]-6-aminohexanoyl]pyrrolidine-2-carbonyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]acetyl]amino]-N-[(2S)-1-[[(2S,3S)-1-amino-3-methyl-1-oxopentan-2-yl]amino]-1-oxopent-4-en-2-yl]pentanediamide Investigative 53325256 C53H87N15O12S 1158.4 CC[C@H](C)[C@@H](C(=O)N)NC(=O)[C@H](CC=C)NC(=O)[C@H](CCC(=O)N)NC(=O)CNC(=O)[C@H](CC1=CN=CN1)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCCN)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CC=C)NC(=O)[C@H](CCSC)NC(=O)C IC50 = 90300 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BU4S0J 4-[(E)-2-(4-Phenyl-1H-imidazol-5-yl)vinyl]pyrimidin-2-amine Investigative 44586869 C15H13N5 263.3 C1=CC=C(C=C1)C2=C(NC=N2)/C=C/C3=NC(=NC=C3)N IC50 = 68000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BU53YX N4-((1-Methyl-4-phenyl-1H-imidazol-5-yl)methyl)pyrimidine-2,4-diamine Investigative 44586901 C15H16N6 280.33 CN1C=NC(=C1CNC2=NC(=NC=C2)N)C3=CC=CC=C3 IC50 ~ 100000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BUKT02 4-[(E)-2-(6-Chloroimidazo[2,1-b][1,3]thiazol-5-yl)ethenyl]pyrimidin-2-amine Investigative 44587325 C11H8ClN5S 277.73 C1=CN=C(N=C1/C=C/C2=C(N=C3N2C=CS3)Cl)N IC50 ~ 100000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BUMX69 (4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-1-Acetylpyrrolidine-2-carbonyl]amino]-3-phenylpropanoyl]amino]-5-amino-5-oxopentanoyl]amino]-5-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-oxopentanoic acid Investigative 137645340 C62H84N16O16 1309.4 CC(C)[C@@H](C(=O)N[C@@H](CC1=CNC2=CC=CC=C21)C(=O)NCC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC3=CC=C(C=C3)O)C(=O)N)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](CC4=CC=CC=C4)NC(=O)[C@@H]5CCCN5C(=O)C IC50 = 129500 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BUO4L7 4-[(E)-2-(6-Phenylimidazo[2,1-b][1,3]thiazol-5-yl)vinyl]pyrimidine Investigative 44586794 C17H12N4S 304.4 C1=CC=C(C=C1)C2=C(N3C=CSC3=N2)/C=C/C4=NC=NC=C4 IC50 ~ 100000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BUPG71 4-N-(4-Chloro-2-fluorophenyl)-6-[(2,5-dimethoxyphenyl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine Investigative 57395925 C21H19ClFN5O2 427.9 COC1=CC(=C(C=C1)OC)CC2=CC3=C(N2)N=C(N=C3NC4=C(C=C(C=C4)Cl)F)N IC50 = 185600 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BW27YB 4-[(E)-2-(1-Methyl-5-phenylimidazol-4-yl)ethenyl]pyrimidin-2-amine Investigative 44586870 C16H15N5 277.32 CN1C=NC(=C1C2=CC=CC=C2)/C=C/C3=NC(=NC=C3)N IC50 ~ 100000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BW3EI4 (2R,3S)-8-[(2S,4R)-5,7-Dihydroxy-2-(4-hydroxyphenyl)-3,4-dihydro-2H-chromen-4-yl]-2-(4-hydroxyphenyl)-3,4-dihydro-2H-chromene-3,5,7-triol Investigative 71521862 C30H26O9 530.5 C1[C@H](C2=C(C=C(C=C2O[C@@H]1C3=CC=C(C=C3)O)O)O)C4=C(C=C(C5=C4O[C@@H]([C@H](C5)O)C6=CC=C(C=C6)O)O)O IC50 = 50000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BW3S6G 6-[(2,4-Dichlorophenyl)methyl]-4-N-[3-(trifluoromethyl)phenyl]-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine Investigative 46886972 C20H14Cl2F3N5 452.3 C1=CC(=CC(=C1)NC2=NC(=NC3=C2C=C(N3)CC4=C(C=C(C=C4)Cl)Cl)N)C(F)(F)F IC50 = 156100 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BW53EL 4-N-(3-Bromophenyl)-7-(naphthalen-2-ylmethyl)pyrrolo[2,3-d]pyrimidine-2,4-diamine Investigative 57396545 C23H18BrN5 444.3 C1=CC=C2C=C(C=CC2=C1)CN3C=CC4=C(N=C(N=C43)N)NC5=CC(=CC=C5)Br IC50 = 50800 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BX30KU 4-N-(4-Chloro-2-fluorophenyl)-6-[(2,4-dichlorophenyl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine Investigative 46886970 C19H13Cl3FN5 436.7 C1=CC(=C(C=C1Cl)Cl)CC2=CC3=C(N2)N=C(N=C3NC4=C(C=C(C=C4)Cl)F)N IC50 = 70900 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BX51DL (3S,6S,9S,14S,17S,23S,26S,29S)-9-[[(2S)-2-Acetamido-4-methylsulfanylbutanoyl]amino]-3-(4-aminobutyl)-N-[(2S,3S)-1-amino-3-methyl-1-oxopentan-2-yl]-17,23-bis(3-amino-3-oxopropyl)-6-[(2S)-butan-2-yl]-26-(1H-imidazol-5-ylmethyl)-2,5,8,12,16,19,22,25,28-nonaoxo-1,4,7,11,15,18,21,24,27-nonazabicyclo[27.3.0]dotriacontane-14-carboxamide Investigative 56656325 C55H90N18O15S 1275.5 CC[C@H](C)[C@H]1C(=O)N[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CC(=O)NC[C@@H](C(=O)N1)NC(=O)[C@H](CCSC)NC(=O)C)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N)CCC(=O)N)CCC(=O)N)CC3=CN=CN3)CCCCN IC50 = 87600 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BX84HQ 4-N-(3-Bromophenyl)-6-[(3,4-dichlorophenyl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine Investigative 3008964 C19H14BrCl2N5 463.2 C1=CC(=CC(=C1)Br)NC2=NC(=NC3=C2C=C(N3)CC4=CC(=C(C=C4)Cl)Cl)N IC50 ~ 50000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BY0PH8 (2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-Acetamidopent-4-enoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-methylpentanoyl]amino]-6-aminohexanoyl]pyrrolidine-2-carbonyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-5-amino-5-oxopentanoyl]amino]acetyl]amino]-N-[(2S)-1-[[(2S)-1-amino-1-oxopent-4-en-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]pentanediamide Investigative 53323499 C59H94N22O14 1335.5 CC[C@H](C)[C@@H](C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC2=CN=CN2)C(=O)N[C@@H](CCC(=O)N)C(=O)NCC(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CC3=CN=CN3)C(=O)N[C@@H](CC=C)C(=O)N)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC=C)NC(=O)C IC50 = 76800 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BZ4F6B 5-[(E)-2-(2-Chloropyrimidin-4-yl)vinyl]-6-phenylimidazo[2,1-b][1,3]thiazole Investigative 11724734 C17H11ClN4S 338.8 C1=CC=C(C=C1)C2=C(N3C=CSC3=N2)/C=C/C4=NC(=NC=C4)Cl IC50 = 66000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BZ53FX 5-(Phenylthio)-9H-pyrimido[4,5-b]indole-2,4-diamine Investigative 25181586 C16H13N5S 307.4 C1=CC=C(C=C1)SC2=CC=CC3=C2C4=C(N=C(N=C4N3)N)N IC50 = 118100 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BZ7A5X (E/Z)-4-(2-(4-Phenyl-1H-pyrazol-5-yl)vinyl)pyrimidin-2-amine Investigative 44586832 C15H13N5 263.3 C1=CC=C(C=C1)C2=C(NN=C2)/C=C/C3=NC(=NC=C3)N IC50 ~ 100000 nM Poor binder T63966 Vascular endothelial growth factor receptor 1 BZ9X0H 4-N-(3-Bromophenyl)-7-[(2-chlorophenyl)methyl]pyrrolo[2,3-d]pyrimidine-2,4-diamine Investigative 57384105 C19H15BrClN5 428.7 C1=CC=C(C(=C1)CN2C=CC3=C(N=C(N=C32)N)NC4=CC(=CC=C4)Br)Cl IC50 = 126300 nM Poor binder