TTD_Target_ID Target_Name TTD_Drug_ID Drug_Name Drug_Highest_Status Drug_PubchemID Molecular_Formula Molecular_Weight Canonical_SMILES Activity Binder_Type T45299 Tissue-type plasminogen activator D07UWV Argatroban Approved 92722 C23H36N6O5S 508.6 C[C@@H]1CCN([C@H](C1)C(=O)O)C(=O)[C@H](CCCN=C(N)N)NS(=O)(=O)C2=CC=CC3=C2NCC(C3)C Ki = 87800 nM Poor binder T45299 Tissue-type plasminogen activator B03ZOI 3-Hydroxy-4-iodo-anthracene-2-carboxylic acid (4-guanidino-phenyl)-amide Investigative 44304098 C22H17IN4O2 496.3 C1=CC=C2C=C3C(=CC2=C1)C=C(C(=C3I)O)C(=O)NC4=CC=C(C=C4)N=C(N)N Ki ~ 95000 nM Poor binder T45299 Tissue-type plasminogen activator B0CO7M N-(5-Phenyl-isoquinolin-1-yl)-guanidine Investigative 44339192 C16H14N4 262.31 C1=CC=C(C=C1)C2=CC=CC3=C2C=CN=C3N=C(N)N Ki = 123900 nM Poor binder T45299 Tissue-type plasminogen activator B0FN8O 2-Carboxyindole-based inhibitor 28 Investigative 10391881 C27H24ClN5O2S 518 C1CN(CCC1NC(=O)C2=CC3=CC=CC=C3N2CC4=NOC(=C4)C5=CC=C(S5)Cl)C6=CC=NC=C6 Ki ~ 100000 nM Poor binder T45299 Tissue-type plasminogen activator B0KAI3 5-[4-[3-(6-Chloro-2-naphthylsulfonyl)propanoyl]piperazino]imidazo[1,2-a]pyridine-2-methanol Investigative 10391715 C25H25ClN4O4S 513 C1CN(CCN1C2=CC=CC3=NC(=CN32)CO)C(=O)CCS(=O)(=O)C4=CC5=C(C=C4)C=C(C=C5)Cl Ki ~ 60000 nM Poor binder T45299 Tissue-type plasminogen activator B0KH8P 4-[(E)-(5-Oxo-2-phenyl-1,3-oxazol-4-ylidene)methyl]benzenecarboximidamide Investigative 16220264 C17H13N3O2 291.3 C1=CC=C(C=C1)C2=N/C(=C/C3=CC=C(C=C3)C(=N)N)/C(=O)O2 IC50 = 68510 nM Poor binder T45299 Tissue-type plasminogen activator B0O7EL 1-Guanidino-7-sulfonamidoisoquinoline 14 Investigative 16658357 C13H14ClN5O4S 371.8 C1=CC2=C(C=C1S(=O)(=O)NCCC(=O)O)C(=NC=C2Cl)N=C(N)N Ki ~ 100000 nM Poor binder T45299 Tissue-type plasminogen activator B0P7CL Cyclic deriv. 35 Investigative 16658183 C16H18ClN5O4S 411.9 C1CCN([C@H](C1)C(=O)O)S(=O)(=O)C2=CC3=C(C=C2)C(=CN=C3N=C(N)N)Cl Ki ~ 100000 nM Poor binder T45299 Tissue-type plasminogen activator B0R3BK 6-Fluoro-2-[2-hydroxy-3-((S)-3-methyl-cyclohexyloxy)-phenyl]-1H-benzoimidazole-5-carboxamidine Investigative 136092211 C21H23FN4O2 382.4 C[C@H]1CCC[C@@H](C1)OC2=CC=CC(=C2O)C3=NC4=C(N3)C=C(C(=C4)C(=N)N)F Ki = 150000 nM Poor binder T45299 Tissue-type plasminogen activator B12YBD N-(4-Guanidino-phenyl)-2-hydroxy-5-methoxy-benzamide Investigative 44304047 C15H16N4O3 300.31 COC1=CC(=C(C=C1)O)C(=O)NC2=CC=C(C=C2)N=C(N)N Ki ~ 95000 nM Poor binder T45299 Tissue-type plasminogen activator B13HLB N-(4-Guanidino-phenyl)-2-hydroxy-4-methyl-benzamide Investigative 44304006 C17H20N4O2 312.37 CC1=CC(=C(C=C1)C(=O)N(C)C2=CC=C(C=C2)N=C(N)N)OC Ki ~ 95000 nM Poor binder T45299 Tissue-type plasminogen activator B15ULK Substituted glycine deriv. 16 Investigative 16658742 C13H14ClN5O4S 371.8 CN(CC(=O)O)S(=O)(=O)C1=CC2=C(C=C1)C(=CN=C2N=C(N)N)Cl Ki ~ 100000 nM Poor binder T45299 Tissue-type plasminogen activator B1P8KG 2-Carboxyindole-based inhibitor 24 Investigative 23647194 C24H25ClN4O2S 469 CC(C)N1CC[C@H](C1)NC(=O)C2=CC3=CC=CC=C3N2CC4=NOC(=C4)C5=CC=C(S5)Cl Ki ~ 100000 nM Poor binder T45299 Tissue-type plasminogen activator B1S9XC N-((1R,2S,5S)-2-(5-Chloro-1H-indole-2-carboxamido)-5-(dimethylcarbamoyl)cyclohexyl)-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-C]pyridine-2-carboxamide Investigative 9808346 C26H31ClN6O3S 543.1 CN1CCC2=C(C1)SC(=N2)C(=O)N[C@@H]3C[C@H](CC[C@@H]3NC(=O)C4=CC5=C(N4)C=CC(=C5)Cl)C(=O)N(C)C Ki = 68200 nM Poor binder T45299 Tissue-type plasminogen activator B27QTA {(R)-2-[2-((S)-1-Formyl-4-guanidino-butylcarbamoyl)-azetidin-1-yl]-1-methyl-2-oxo-1-phenyl-ethyl}-carbamic acid tert-butyl ester Investigative 10814863 C24H36N6O5 488.6 C[C@@](C1=CC=CC=C1)(C(=O)N2CC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C=O)NC(=O)OC(C)(C)C IC50 = 120000 nM Poor binder T45299 Tissue-type plasminogen activator B27WSD (2S)-N-Cyclopentyl-N-methyl-5-[4-(methylamino)phenyl]-2-[(4-propylphenyl)sulfonylamino]pent-4-ynamide Investigative 10390481 C27H35N3O3S 481.7 CCCC1=CC=C(C=C1)S(=O)(=O)N[C@@H](CC#CC2=CC=C(C=C2)NC)C(=O)N(C)C3CCCC3 Ki = 190000 nM Poor binder T45299 Tissue-type plasminogen activator B28LHJ (17S,20R)-20-(Benzylsulfonylamino)-N-[(4-carbamimidoylphenyl)methyl]-3,10,19-trioxo-2,5,8,11,18-pentazatetracyclo[20.2.2.25,8.212,15]triaconta-1(25),12,14,22(26),23,27-hexaene-17-carboxamide;2,2,2-trifluoroacetic acid Investigative 71720404 C43H48F3N9O8S 908 C1CN2CCN1CC(=O)NC3=CC=C(C[C@H](C(=O)N[C@@H](CC4=CC=C(C=C4)NC(=O)C2)C(=O)NCC5=CC=C(C=C5)C(=N)N)NS(=O)(=O)CC6=CC=CC=C6)C=C3.C(=O)(C(F)(F)F)O Ki ~ 100000 nM Poor binder T45299 Tissue-type plasminogen activator B28OHJ Ethyl 1-(diphenoxyphosphoryl)-2-(4-guanidinophenyl)ethylcarbamate Investigative 16718712 C24H27N4O5P 482.5 CCOC(=O)NC(CC1=CC=C(C=C1)N=C(N)N)P(=O)(OC2=CC=CC=C2)OC3=CC=CC=C3 IC50 = 57000 nM Poor binder T45299 Tissue-type plasminogen activator B2KWI7 N-Isoquinolin-1-yl-guanidine Investigative 18771297 C10H10N4 186.21 C1=CC=C2C(=C1)C=CN=C2N=C(N)N Ki = 126200 nM Poor binder T45299 Tissue-type plasminogen activator B2P6IQ 6-Fluoro-2-[2-hydroxy-3-(4-methyl-cyclohexyloxy)-phenyl]-1H-benzoimidazole-5-carboxamidine Investigative 136092209 C21H23FN4O2 382.4 CC1CCC(CC1)OC2=CC=CC(=C2O)C3=NC4=C(N3)C=C(C(=C4)C(=N)N)F Ki = 71000 nM Poor binder T45299 Tissue-type plasminogen activator B2R6WK 3-[(R)-3-[4-(2-Hydroxy-ethyl)-piperazin-1-yl]-2-(naphthalene-2-sulfonylamino)-3-oxo-propyl]-benzamidine Investigative 10815545 C26H31N5O4S 509.6 C1CN(CCN1CCO)C(=O)[C@@H](CC2=CC(=CC=C2)C(=N)N)NS(=O)(=O)C3=CC4=CC=CC=C4C=C3 Ki = 180000 nM Poor binder T45299 Tissue-type plasminogen activator B2TWQ0 N-(4-Chloro-isoquinolin-1-yl)-guanidine Investigative 44339231 C10H9ClN4 220.66 C1=CC=C2C(=C1)C(=CN=C2N=C(N)N)Cl Ki = 128500 nM Poor binder T45299 Tissue-type plasminogen activator B30SGZ 6-Carbamimidoyl-naphthalene-2-carboxylic acid (3,5-dimethoxy-phenyl)-amide Investigative 11450922 C20H19N3O3 349.4 COC1=CC(=CC(=C1)NC(=O)C2=CC3=C(C=C2)C=C(C=C3)C(=N)N)OC IC50 ~ 62000 nM Poor binder T45299 Tissue-type plasminogen activator B3K9LO 3-[(R)-3-(4-Formyl-piperazin-1-yl)-2-(naphthalene-2-sulfonylamino)-3-oxo-propyl]-benzamidine Investigative 10624997 C25H27N5O4S 493.6 C1CN(CCN1C=O)C(=O)[C@@H](CC2=CC(=CC=C2)C(=N)N)NS(=O)(=O)C3=CC4=CC=CC=C4C=C3 Ki = 110000 nM Poor binder T45299 Tissue-type plasminogen activator B3LRT9 N-[2'-(Aminosulfonyl)-4-biphenylyl]-Nalpha-(3-amidinobenzoyl)-D-phenylglycinamide Investigative 44330879 C28H25N5O4S 527.6 C1=CC=C(C=C1)[C@H](C(=O)NC2=CC=C(C=C2)C3=CC=CC=C3S(=O)(=O)N)NC(=O)C4=CC=CC(=C4)C(=N)N IC50 ~ 180000 nM Poor binder T45299 Tissue-type plasminogen activator B3M5YL 3-(6-Chloronaphthalen-2-yl)sulfonyl-N-methyl-N-[1-(2-methylpyridin-4-yl)piperidin-4-yl]propanamide Investigative 10117027 C25H28ClN3O3S 486 CC1=NC=CC(=C1)N2CCC(CC2)N(C)C(=O)CCS(=O)(=O)C3=CC4=C(C=C3)C=C(C=C4)Cl Ki = 67000 nM Poor binder T45299 Tissue-type plasminogen activator B3W0VJ 2-(4-Diethylamino-2-hydroxy-phenyl)-1H-benzoimidazole-5-carboxamidine Investigative 135544579 C18H21N5O 323.4 CCN(CC)C1=CC(=C(C=C1)C2=NC3=C(N2)C=C(C=C3)C(=N)N)O Ki = 100000 nM Poor binder T45299 Tissue-type plasminogen activator B3XE7D 8-(Pyrimidin-2-ylamino)-6-((E)-styryl)-naphthalene-2-carboxamidine Investigative 44392403 C23H19N5 365.4 C1=CC=C(C=C1)/C=C/C2=CC(=C3C=C(C=CC3=C2)C(=N)N)NC4=NC=CC=N4 Ki ~ 50000 nM Poor binder T45299 Tissue-type plasminogen activator B4A5KU 4-Bromo-3-hydroxy-anthracene-2-carboxylic acid (4-guanidino-phenyl)-amide Investigative 44304099 C22H17BrN4O2 449.3 C1=CC=C2C=C3C(=CC2=C1)C=C(C(=C3Br)O)C(=O)NC4=CC=C(C=C4)N=C(N)N Ki ~ 95000 nM Poor binder T45299 Tissue-type plasminogen activator B4AQ2J Substituted glycine deriv. 30 Investigative 16658031 C16H18ClN5O5S 427.9 C1COCCC1(C(=O)O)NS(=O)(=O)C2=CC3=C(C=C2)C(=CN=C3N=C(N)N)Cl Ki ~ 100000 nM Poor binder T45299 Tissue-type plasminogen activator B4CQ1W 2-[3-(Phenylethynyl)-5-chloro-2-pyridinyl]guanidine Investigative 44298525 C14H11ClN4 270.72 C1=CC=C(C=C1)C#CC2=C(N=CC(=C2)Cl)N=C(N)N Ki = 65900 nM Poor binder T45299 Tissue-type plasminogen activator B4EIL5 Diphenyl 1-(N-benzyloxycarbonylamino)-1-(4-amidinophenyl)propanephosphonate Investigative 24748791 C30H30N3O5P 543.5 C1=CC=C(C=C1)COC(=O)NC(CCC2=CC=C(C=C2)C(=N)N)P(=O)(OC3=CC=CC=C3)OC4=CC=CC=C4 IC50 = 68000 nM Poor binder T45299 Tissue-type plasminogen activator B4EZ5H N-(5-Bromo-isoquinolin-1-yl)-guanidine Investigative 44339233 C10H9BrN4 265.11 C1=CC2=C(C=CN=C2N=C(N)N)C(=C1)Br Ki = 140100 nM Poor binder T45299 Tissue-type plasminogen activator B4UZ2R 6-Fluoro-2-(2-hydroxy-3-isobutoxy-phenyl)-1H-benzoimidazole-5-carboxamidine Investigative 445847 C18H19FN4O2 342.4 CC(C)COC1=CC=CC(=C1O)C2=NC3=C(N2)C=C(C(=C3)C(=N)N)F Ki = 61000 nM Poor binder T45299 Tissue-type plasminogen activator B54PRQ Benzyl 2-[[6-amino-3-chloro-5-[(Z)-N'-hydroxycarbamimidoyl]pyrazin-2-yl]amino]acetate Investigative 136266885 C14H15ClN6O3 350.76 C1=CC=C(C=C1)COC(=O)CNC2=NC(=C(N=C2Cl)/C(=N/O)/N)N IC50 = 200000 nM Poor binder T45299 Tissue-type plasminogen activator B5DCY2 1-(2-Amino-3,3-dicyclohexyl-propionyl)-pyrrolidine-2-carboxylic acid (4-amino-cyclohexylmethyl)-amide Investigative 10367012 C27H48N4O2 460.7 C1CCC(CC1)C(C2CCCCC2)[C@H](C(=O)N3CCC[C@H]3C(=O)NCC4CCC(CC4)N)N Ki = 137000 nM Poor binder T45299 Tissue-type plasminogen activator B5JE7T N-(4-Guanidino-phenyl)-2-hydroxy-3-methyl-benzamide Investigative 44304353 C15H16N4O2 284.31 CC1=C(C(=CC=C1)C(=O)NC2=CC=C(C=C2)N=C(N)N)O Ki ~ 95000 nM Poor binder T45299 Tissue-type plasminogen activator B5PJX1 2-(3-Methoxy-2-hydroxyphenyl)-1H-benzimidazole-5-carboxamidine Investigative 135427245 C15H14N4O2 282.3 COC1=CC=CC(=C1O)C2=NC3=C(N2)C=C(C=C3)C(=N)N Ki = 69000 nM Poor binder T45299 Tissue-type plasminogen activator B5VJ7P (2S)-N-[(2S)-5-(Diaminomethylideneamino)-1-oxopentan-2-yl]-1-[(2R)-2-phenyl-2-[(2,2,2-trifluoroacetyl)amino]propanoyl]azetidine-2-carboxamide Investigative 10791027 C21H27F3N6O4 484.5 C[C@@](C1=CC=CC=C1)(C(=O)N2CC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C=O)NC(=O)C(F)(F)F IC50 = 130000 nM Poor binder T45299 Tissue-type plasminogen activator B64SUE 1-Guanidino-7-sulfonamidoisoquinoline 12 Investigative 16658356 C17H14ClN5O4S 419.8 C1=CC(=CC(=C1)NS(=O)(=O)C2=CC3=C(C=C2)C(=CN=C3N=C(N)N)Cl)C(=O)O Ki ~ 100000 nM Poor binder T45299 Tissue-type plasminogen activator B67YGB 2-(1-(3-(6-Chloronaphthalen-2-ylsulfonyl)propanoyl)piperidin-4-yl)-5-methyl-1H-imidazo[1,5-c]imidazol-3(2H)-one Investigative 9935746 C24H25ClN4O4S 501 CC1=NC=C2N1C(=O)N(C2)C3CCN(CC3)C(=O)CCS(=O)(=O)C4=CC5=C(C=C4)C=C(C=C5)Cl Ki ~ 60000 nM Poor binder T45299 Tissue-type plasminogen activator B6MQT3 N-(4-Amidinophenyl)-2-hydroxy-3-phenylbenzamide Investigative 44303804 C20H17N3O2 331.4 C1=CC=C(C=C1)C2=C(C(=CC=C2)C(=O)NC3=CC=C(C=C3)C(=N)N)O Ki = 53000 nM Poor binder T45299 Tissue-type plasminogen activator B6VSZ1 3-Hydroxy-4-methoxy-anthracene-2-carboxylic acid (6-guanidino-pyridin-3-yl)-amide Investigative 44303935 C22H19N5O3 401.4 COC1=C(C(=CC2=CC3=CC=CC=C3C=C21)C(=O)NC4=CN=C(C=C4)N=C(N)N)O Ki = 150000 nM Poor binder T45299 Tissue-type plasminogen activator B78ZBK N-(4-Guanidino-phenyl)-2-hydroxy-benzamide Investigative 44303733 C14H14N4O2 270.29 C1=CC=C(C(=C1)C(=O)NC2=CC=C(C=C2)N=C(N)N)O Ki ~ 95000 nM Poor binder T45299 Tissue-type plasminogen activator B7R5UJ 1-{[5-(5-Chloro-2-thienyl)isoxazol-3-YL]methyl}-N-(1-isopropylpiperidin-4-YL)-1H-indole-2-carboxamide Investigative 6540265 C25H27ClN4O2S 483 CC(C)N1CCC(CC1)NC(=O)C2=CC3=CC=CC=C3N2CC4=NOC(=C4)C5=CC=C(S5)Cl Ki ~ 100000 nM Poor binder T45299 Tissue-type plasminogen activator B7W3KD 2-Biphenyl-3-yl-1H-indole-5-carboxamidine Investigative 10946869 C21H17N3 311.4 C1=CC=C(C=C1)C2=CC(=CC=C2)C3=CC4=C(N3)C=CC(=C4)C(=N)N Ki = 138000 nM Poor binder T45299 Tissue-type plasminogen activator B7ZB9U 2-[3-[(E)-2-Cyclohexylethenyl]-5-chloro-2-pyridinyl]guanidine Investigative 44298523 C14H19ClN4 278.78 C1CCC(CC1)/C=C/C2=C(N=CC(=C2)Cl)N=C(N)N Ki = 71500 nM Poor binder T45299 Tissue-type plasminogen activator B87OAE Diphenyl N-(benzyloxycarbonyl)amino(4-amidinophenyl)methanephosphonate Investigative 9827867 C28H26N3O5P 515.5 C1=CC=C(C=C1)COC(=O)NC(C2=CC=C(C=C2)C(=N)N)P(=O)(OC3=CC=CC=C3)OC4=CC=CC=C4 IC50 = 66000 nM Poor binder T45299 Tissue-type plasminogen activator B8AFI9 4-Chloro-N-(4-guanidino-phenyl)-2-hydroxy-benzamide Investigative 44304046 C14H13ClN4O2 304.73 C1=CC(=CC=C1NC(=O)C2=C(C=C(C=C2)Cl)O)N=C(N)N Ki ~ 95000 nM Poor binder T45299 Tissue-type plasminogen activator B8M4EP 5-Bromo-N-(4-guanidino-phenyl)-2-hydroxy-benzamide Investigative 44303719 C14H13BrN4O2 349.18 C1=CC(=CC=C1NC(=O)C2=C(C=CC(=C2)Br)O)N=C(N)N Ki ~ 95000 nM Poor binder T45299 Tissue-type plasminogen activator B8VYZ0 Benzyl 2-[[6-amino-3-chloro-5-(diaminomethylidenecarbamoyl)pyrazin-2-yl]amino]acetate Investigative 57404503 C15H16ClN7O3 377.78 C1=CC=C(C=C1)COC(=O)CNC2=NC(=C(N=C2Cl)C(=O)N=C(N)N)N IC50 ~ 190000 nM Poor binder T45299 Tissue-type plasminogen activator B9EMP4 2-[[4-Chloro-1-(diaminomethylideneamino)isoquinolin-7-yl]sulfonylamino]benzoic Acid Investigative 11419694 C17H14ClN5O4S 419.8 C1=CC=C(C(=C1)C(=O)O)NS(=O)(=O)C2=CC3=C(C=C2)C(=CN=C3N=C(N)N)Cl Ki ~ 100000 nM Poor binder T45299 Tissue-type plasminogen activator B9GZ5S 7-Methoxy-8-[1-(methylsulfonyl)-1H-pyrazol-4-YL]naphthalene-2-carboximidamide Investigative 5289529 C16H16N4O3S 344.4 COC1=C(C2=C(C=CC(=C2)C(=N)N)C=C1)C3=CN(N=C3)S(=O)(=O)C Ki ~ 100000 nM Poor binder T45299 Tissue-type plasminogen activator B9VGY7 3-Hydroxy-4-methoxy-anthracene-2-carboxylic acid (4-guanidino-phenyl)-amide Investigative 44304097 C23H20N4O3 400.4 COC1=C(C(=CC2=CC3=CC=CC=C3C=C21)C(=O)NC4=CC=C(C=C4)N=C(N)N)O Ki = 181000 nM Poor binder T45299 Tissue-type plasminogen activator B9WVZ2 2-[3-[(E)-Styryl]-5-chloro-2-pyridinyl]guanidine Investigative 44298524 C14H13ClN4 272.73 C1=CC=C(C=C1)/C=C/C2=C(N=CC(=C2)Cl)N=C(N)N Ki = 53800 nM Poor binder T45299 Tissue-type plasminogen activator BA6QC9 N-(4-Carbamimidoyl-phenyl)-2-hydroxy-5-nitro-benzamide Investigative 44303808 C14H12N4O4 300.27 C1=CC(=CC=C1C(=N)N)NC(=O)C2=C(C=CC(=C2)[N+](=O)[O-])O Ki = 94000 nM Poor binder T45299 Tissue-type plasminogen activator BAM0E8 6-Fluoro-2-[2-hydroxy-3-((S)-2-methyl-cyclohexyloxy)-phenyl]-1H-benzoimidazole-5-carboxamidine Investigative 447540 C21H23FN4O2 382.4 C[C@@H]1CCCC[C@@H]1OC2=CC=CC(=C2O)C3=NC4=C(N3)C=C(C(=C4)C(=N)N)F Ki = 58000 nM Poor binder T45299 Tissue-type plasminogen activator BB16XW 2-{5-[Amino(iminio)methyl]-1H-benzimidazol-2-YL}benzenolate Investigative 1506 C14H12N4O 252.27 C1=CC=C(C(=C1)C2=NC3=C(N2)C=C(C=C3)C(=N)N)O Ki = 75000 nM Poor binder T45299 Tissue-type plasminogen activator BB1FV3 3-[(E)-2-(5-Chloro-2-guanidino-pyridin-3-yl)-vinyl]-benzoic acid Investigative 9948854 C15H13ClN4O2 316.74 C1=CC(=CC(=C1)C(=O)O)/C=C/C2=C(N=CC(=C2)Cl)N=C(N)N Ki = 52000 nM Poor binder T45299 Tissue-type plasminogen activator BB7C6R (S)-1-(9-Hydroxy-9H-3-aza-fluorene-9-carbonyl)-pyrrolidine-2-carboxylic acid 2-aminomethyl-5-chloro-benzylamide Investigative 11317532 C26H25ClN4O3 477 C1C[C@H](N(C1)C(=O)C2(C3=C(C=NC=C3)C4=CC=CC=C42)O)C(=O)NCC5=C(C=CC(=C5)Cl)CN Ki ~ 100000 nM Poor binder T45299 Tissue-type plasminogen activator BBY1C6 4-Ethoxy-N-(4-guanidino-phenyl)-2-hydroxy-benzamide Investigative 44303824 C16H18N4O3 314.34 CCOC1=CC(=C(C=C1)C(=O)NC2=CC=C(C=C2)N=C(N)N)O Ki ~ 95000 nM Poor binder T45299 Tissue-type plasminogen activator BBYR96 2-Carboxyindole-based inhibitor 33 Investigative 23647198 C25H20ClN5O2S 490 C1C(CN1C2=CC=NC=C2)NC(=O)C3=CC4=CC=CC=C4N3CC5=NOC(=C5)C6=CC=C(S6)Cl Ki ~ 100000 nM Poor binder T45299 Tissue-type plasminogen activator BCAL64 3-Hydroxy-anthracene-2-carboxylic acid (4-guanidino-phenyl)-amide Investigative 44304104 C22H18N4O2 370.4 C1=CC=C2C=C3C=C(C(=CC3=CC2=C1)C(=O)NC4=CC=C(C=C4)N=C(N)N)O Ki ~ 95000 nM Poor binder T45299 Tissue-type plasminogen activator BDT3P2 Substituted glycine deriv. 17 Investigative 16658407 C18H16ClN5O4S 433.9 C1=CC=C(C=C1)N(CC(=O)O)S(=O)(=O)C2=CC3=C(C=C2)C(=CN=C3N=C(N)N)Cl Ki ~ 100000 nM Poor binder T45299 Tissue-type plasminogen activator BF6XK1 2-(5-Nitro-2-hydroxyphenyl)-1H-benzimidazole-5-carboxamidine Investigative 135407736 C14H11N5O3 297.27 C1=CC2=C(C=C1C(=N)N)NC(=N2)C3=C(C=CC(=C3)[N+](=O)[O-])O Ki = 56000 nM Poor binder T45299 Tissue-type plasminogen activator BG8FM0 1-{2-[(4-Chlorophenyl)amino]-2-oxoethyl}-N-(1-isopropylpiperidin-4-YL)-1H-indole-2-carboxamide Investigative 6540268 C25H29ClN4O2 453 CC(C)N1CCC(CC1)NC(=O)C2=CC3=CC=CC=C3N2CC(=O)NC4=CC=C(C=C4)Cl Ki ~ 100000 nM Poor binder T45299 Tissue-type plasminogen activator BGI97R 2-(2-Hydroxy-3-ethoxyphenyl)-6-chloro-1H-benzimidazole-5-carboxamidine Investigative 136092208 C16H15ClN4O2 330.77 CCOC1=CC=CC(=C1O)C2=NC3=C(N2)C=C(C(=C3)C(=N)N)Cl Ki ~ 75000 nM Poor binder T45299 Tissue-type plasminogen activator BGQ9K3 6-Carbamimidoyl-naphthalene-2-carboxylic acid (4-carbamoyl-phenyl)-amide Investigative 11244460 C19H16N4O2 332.4 C1=CC(=CC=C1C(=O)N)NC(=O)C2=CC3=C(C=C2)C=C(C=C3)C(=N)N Ki ~ 100000 nM Poor binder T45299 Tissue-type plasminogen activator BH3QG6 2-Carboxyindole-based inhibitor 13 Investigative 20801121 C25H25ClN4O2S 481 C1CC1N2CCC(CC2)NC(=O)C3=CC4=CC=CC=C4N3CC5=NOC(=C5)C6=CC=C(S6)Cl Ki ~ 100000 nM Poor binder T45299 Tissue-type plasminogen activator BHL7S1 6-Carbamimidoyl-naphthalene-2-carboxylic acid (4-ethyl-phenyl)-amide Investigative 11347670 C20H19N3O 317.4 CCC1=CC=C(C=C1)NC(=O)C2=CC3=C(C=C2)C=C(C=C3)C(=N)N Ki = 83900 nM Poor binder T45299 Tissue-type plasminogen activator BHS98V 2-(2-Hydroxy-3-ethoxyphenyl)-6-fluoro-1H-benzimidazole-5-carboxamidine Investigative 136092214 C16H15FN4O2 314.31 CCOC1=CC=CC(=C1O)C2=NC3=C(N2)C=C(C(=C3)C(=N)N)F Ki ~ 75000 nM Poor binder T45299 Tissue-type plasminogen activator BI1R2Q Benzyl 2-[(6-amino-5-carbamimidoyl-3-chloropyrazin-2-yl)amino]acetate Investigative 57404502 C14H15ClN6O2 334.76 C1=CC=C(C=C1)COC(=O)CNC2=NC(=C(N=C2Cl)C(=N)N)N IC50 = 200000 nM Poor binder T45299 Tissue-type plasminogen activator BI5U8S 6-(2-Phenylcyclopropyl)naphthalene-2-carboximidamide Investigative 21707065 C20H18N2 286.4 C1C(C1C2=CC3=C(C=C2)C=C(C=C3)C(=N)N)C4=CC=CC=C4 Ki = 69110 nM Poor binder T45299 Tissue-type plasminogen activator BI6HN2 2-Carboxyindole-based inhibitor 7 Investigative 20801139 C23H23ClN4O2S 455 CN1CCC(CC1)NC(=O)C2=CC3=CC=CC=C3N2CC4=NOC(=C4)C5=CC=C(S5)Cl Ki ~ 100000 nM Poor binder T45299 Tissue-type plasminogen activator BI97QF Chembl2332610 Investigative 71716976 C64H93N17O16S3 1452.7 C[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CSCC2=CC3=CC(=C2)CSC[C@@H](C(=O)NCC(=O)NCC(=O)N[C@H](C(=O)N4CCC[C@H]4C(=O)N[C@@H](CSC3)C(=O)N5CCC[C@H]5C(=O)N6CCC[C@H]6C(=O)N1)CCCN=C(N)N)NC(=O)[C@H](CO)N)C(=O)N[C@@H](CCCCN)C(=O)O)CC7=CC=C(C=C7)O Ki ~ 120000 nM Poor binder T45299 Tissue-type plasminogen activator BIY84V 2-(2-Hydroxy-biphenyl-3-yl)-3-methyl-3H-benzoimidazole-5-carboxamidine Investigative 135535997 C21H18N4O 342.4 CN1C2=C(C=CC(=C2)C(=N)N)N=C1C3=CC=CC(=C3O)C4=CC=CC=C4 Ki = 150000 nM Poor binder T45299 Tissue-type plasminogen activator BJ3RV5 1H-Indole-1-acetamide,N-(5-chloro-2-pyridinyl)-2-[[[1-(1-methylethyl)-4-piperidinyl]amino]carbonyl]- Investigative 10095455 C24H28ClN5O2 454 CC(C)N1CCC(CC1)NC(=O)C2=CC3=CC=CC=C3N2CC(=O)NC4=NC=C(C=C4)Cl Ki ~ 100000 nM Poor binder T45299 Tissue-type plasminogen activator BJ5GN1 3-Chloro-N-(4-guanidino-phenyl)-2-hydroxy-benzamide Investigative 44304192 C14H13ClN4O2 304.73 C1=CC(=C(C(=C1)Cl)O)C(=O)NC2=CC=C(C=C2)N=C(N)N Ki = 95000 nM Poor binder T45299 Tissue-type plasminogen activator BK3BX5 2-(5-Methyl-2-hydroxyphenyl)-1H-benzimidazole-5-carboxamidine Investigative 135443730 C15H14N4O 266.3 CC1=CC(=C(C=C1)O)C2=NC3=C(N2)C=C(C=C3)C(=N)N Ki = 113000 nM Poor binder T45299 Tissue-type plasminogen activator BK5SO7 Substituted glycine deriv. 29 Investigative 9802514 C17H20ClN5O4S 425.9 C1CCC(CC1)(C(=O)O)NS(=O)(=O)C2=CC3=C(C=C2)C(=CN=C3N=C(N)N)Cl Ki ~ 100000 nM Poor binder T45299 Tissue-type plasminogen activator BK75XF Naphthalene-2-carboximidamide Investigative 193409 C11H10N2 170.21 C1=CC=C2C=C(C=CC2=C1)C(=N)N Ki ~ 100000 nM Poor binder T45299 Tissue-type plasminogen activator BKS48Q N-[2-(3-Amidinophenoxy)ethyl]-2'-sulfamoylbiphenyl-4-carboxamide Investigative 9954812 C22H22N4O4S 438.5 C1=CC=C(C(=C1)C2=CC=C(C=C2)C(=O)NCCOC3=CC=CC(=C3)C(=N)N)S(=O)(=O)N IC50 = 109000 nM Poor binder T45299 Tissue-type plasminogen activator BL0O2Q N-Butyl-3-[[4-(diaminomethylideneamino)phenyl]methylamino]imidazo[1,2-a]pyridine-7-carboxamide Investigative 127041472 C20H25N7O 379.5 CCCCNC(=O)C1=CC2=NC=C(N2C=C1)NCC3=CC=C(C=C3)N=C(N)N IC50 ~ 100000 nM Poor binder T45299 Tissue-type plasminogen activator BL7R2B 3-[(R)-3-(4-Methanesulfonyl-piperazin-1-yl)-2-(naphthalene-2-sulfonylamino)-3-oxo-propyl]-benzamidine Investigative 10816339 C25H29N5O5S2 543.7 CS(=O)(=O)N1CCN(CC1)C(=O)[C@@H](CC2=CC(=CC=C2)C(=N)N)NS(=O)(=O)C3=CC4=CC=CC=C4C=C3 Ki = 190000 nM Poor binder T45299 Tissue-type plasminogen activator BLQ3J7 N-(7-Phenyl-isoquinolin-1-yl)-guanidine Investigative 44339270 C16H14N4 262.31 C1=CC=C(C=C1)C2=CC3=C(C=C2)C=CN=C3N=C(N)N Ki = 123900 nM Poor binder T45299 Tissue-type plasminogen activator BM4CJ5 N-(6-Carbamimidoyl-naphthalen-2-yl)-benzamide Investigative 11149953 C18H12N2O 272.3 C1=CC=C(C=C1)C(=O)NC2=CC3=C(C=C2)C=C(C=C3)C#N Ki ~ 100000 nM Poor binder T45299 Tissue-type plasminogen activator BM6ND8 Chembl2332604 Investigative 71716975 C59H82N16O15S3 1351.6 C[C@H]1C(=O)N[C@H](C(=O)N[C@@H](CSCC2=CC3=CC(=C2)CSC[C@@H](C(=O)NCC(=O)NCC(=O)N[C@H](C(=O)N4CCC[C@H]4C(=O)N[C@@H](CSC3)C(=O)N5CCC[C@H]5C(=O)N6CCC[C@H]6C(=O)N1)CCCN=C(N)N)NC(=O)CN)C(=O)NCC(=O)O)CC7=CC=C(C=C7)O Ki ~ 120000 nM Poor binder T45299 Tissue-type plasminogen activator BND4O9 (2S)-N-[(2S)-5-(Diaminomethylideneamino)-1-oxopentan-2-yl]-1-[(2R)-2-phenyl-2-[(2,2,2-trifluoroacetyl)amino]butanoyl]azetidine-2-carboxamide Investigative 10791461 C22H29F3N6O4 498.5 CC[C@@](C1=CC=CC=C1)(C(=O)N2CC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C=O)NC(=O)C(F)(F)F IC50 = 62000 nM Poor binder T45299 Tissue-type plasminogen activator BNV7U9 2-(5-Methoxy-2-hydroxyphenyl)-1H-benzimidazole-5-carboxamidine Investigative 1503 C15H14N4O2 282.3 COC1=CC(=C(C=C1)O)C2=NC3=C(N2)C=C(C=C3)C(=N)N Ki = 63000 nM Poor binder T45299 Tissue-type plasminogen activator BO9SZ8 2-(1-(3-(6-Chloronaphthalen-2-ylsulfonyl)propanoyl)piperidin-4-yl)-5-(hydroxymethyl)-1H-imidazo[1,5-c]imidazol-3(2H)-one Investigative 10324263 C24H25ClN4O5S 517 C1CN(CCC1N2CC3=CN=C(N3C2=O)CO)C(=O)CCS(=O)(=O)C4=CC5=C(C=C4)C=C(C=C5)Cl Ki ~ 60000 nM Poor binder T45299 Tissue-type plasminogen activator BOI71W N-[(4-Chloro-1-guanidino-7-isoquinolinyl)sulphonyl]-N-(cyclopentylmethyl)glycine Investigative 16658408 C18H22ClN5O4S 439.9 C1CCC(C1)CN(CC(=O)O)S(=O)(=O)C2=CC3=C(C=C2)C(=CN=C3N=C(N)N)Cl Ki ~ 100000 nM Poor binder T45299 Tissue-type plasminogen activator BP4G7N Cyclic deriv. 34 Investigative 16658181 C15H16ClN5O4S 397.8 C1C[C@H](N(C1)S(=O)(=O)C2=CC3=C(C=C2)C(=CN=C3N=C(N)N)Cl)C(=O)O Ki ~ 100000 nM Poor binder T45299 Tissue-type plasminogen activator BP6EM8 N-Methyl-2-[[[[(2-naphthyl)sulfonyl]amino]acetyl]amino]-3-[3-(diaminomethyl)phenyl]propanamide Investigative 44367355 C23H27N5O4S 469.6 CNC(=O)C(CC1=CC(=CC=C1)C(N)N)NC(=O)CNS(=O)(=O)C2=CC3=CC=CC=C3C=C2 Ki = 69000 nM Poor binder T45299 Tissue-type plasminogen activator BP81YN 2-(3-Methyl-2-hydroxyphenyl)-1H-benzimidazole-5-carboxamidine Investigative 135501618 C15H14N4O 266.3 CC1=C(C(=CC=C1)C2=NC3=C(N2)C=C(C=C3)C(=N)N)O Ki = 69000 nM Poor binder T45299 Tissue-type plasminogen activator BPC7D8 2-Carboxyindole 17 Investigative 20801160 C26H28ClN3OS 466 CC(C)N1CCC(CC1)NC(=O)C2=CC3=CC=CC=C3N2CC4=CC5=C(S4)C=C(C=C5)Cl Ki ~ 100000 nM Poor binder T45299 Tissue-type plasminogen activator BPD92J N-(4-Guanidino-phenyl)-2-hydroxy-5-methyl-benzamide Investigative 44303839 C15H16N4O2 284.31 CC1=CC(=C(C=C1)O)C(=O)NC2=CC=C(C=C2)N=C(N)N Ki ~ 95000 nM Poor binder T45299 Tissue-type plasminogen activator BQHU17 N-(4-Bromo-isoquinolin-1-yl)-guanidine Investigative 44339232 C10H9BrN4 265.11 C1=CC=C2C(=C1)C(=CN=C2N=C(N)N)Br Ki = 159200 nM Poor binder T45299 Tissue-type plasminogen activator BR1ZG9 2-Hydroxy-biphenyl-3-carboxylic acid (4-guanidino-phenyl)-amide Investigative 44304105 C20H18N4O2 346.4 C1=CC=C(C=C1)C2=C(C(=CC=C2)C(=O)NC3=CC=C(C=C3)N=C(N)N)O Ki ~ 95000 nM Poor binder T45299 Tissue-type plasminogen activator BR56DV N-[1-(3-Diaminomethyl-benzyl)-2-oxo-2-piperidin-1-yl-ethyl]-4-methyl-benzenesulfonamide Investigative 44367444 C22H30N4O3S 430.6 CC1=CC=C(C=C1)S(=O)(=O)NC(CC2=CC(=CC=C2)C(N)N)C(=O)N3CCCCC3 Ki = 120000 nM Poor binder T45299 Tissue-type plasminogen activator BRXD81 Diphenyl 1-(benzoylamino)-2-(4-guanidinophenyl)-ethanephosphonate Investigative 16718807 C28H27N4O4P 514.5 C1=CC=C(C=C1)C(=O)NC(CC2=CC=C(C=C2)N=C(N)N)P(=O)(OC3=CC=CC=C3)OC4=CC=CC=C4 IC50 = 125000 nM Poor binder T45299 Tissue-type plasminogen activator BS65JA Substituted glycine deriv. 23 Investigative 16657879 C15H18ClN5O4S 399.9 CC(C)[C@@H](C(=O)O)NS(=O)(=O)C1=CC2=C(C=C1)C(=CN=C2N=C(N)N)Cl Ki ~ 100000 nM Poor binder T45299 Tissue-type plasminogen activator BSAX59 6-Carbamimidoyl-N-[1-(2-methylpropyl)-1,2,3,4-tetrahydroisoquinolin-7-yl]naphthalene-2-carboxamide Investigative 11188793 C25H28N4O 400.5 CC(C)CC1C2=C(CCN1)C=CC(=C2)NC(=O)C3=CC4=C(C=C3)C=C(C=C4)C(=N)N Ki ~ 50000 nM Poor binder T45299 Tissue-type plasminogen activator BSCM59 6-[N-(4-(Aminomethyl)phenyl)carbamyl]-2-naphthalenecarboxamidine Investigative 447733 C19H18N4O 318.4 C1=CC(=CC=C1CN)NC(=O)C2=CC3=C(C=C2)C=C(C=C3)C(=N)N Ki = 58400 nM Poor binder T45299 Tissue-type plasminogen activator BSE63D 1-({4-Chloro-1-[(Diaminomethylidene)amino]isoquinolin-7-Yl}sulfonyl)-D-Proline Investigative 9843775 C15H16ClN5O4S 397.8 C1C[C@@H](N(C1)S(=O)(=O)C2=CC3=C(C=C2)C(=CN=C3N=C(N)N)Cl)C(=O)O Ki ~ 100000 nM Poor binder T45299 Tissue-type plasminogen activator BTYL37 2-Carboxyindole-based inhibitor 31 Investigative 22394409 C27H24ClN5O2S 518 C1CN(CCC1NC2=CC=NC=C2)C(=O)C3=CC4=CC=CC=C4N3CC5=NOC(=C5)C6=CC=C(S6)Cl Ki = 64010 nM Poor binder T45299 Tissue-type plasminogen activator BU38EA Cycloleucine deriv. 43 Investigative 16658290 C18H23ClN6O4S 454.9 C1CCC(C1)(C(=O)NCCO)NS(=O)(=O)C2=CC3=C(C=C2)C(=CN=C3N=C(N)N)Cl Ki = 108000 nM Poor binder T45299 Tissue-type plasminogen activator BUM8R9 (3S)-N-[2'-(Aminosulfonyl)-4-biphenylyl]-2-(3-amidinobenzoyl)-1,2,3,4-tetrahydroisoquinoline-3alpha-carboxamide Investigative 44331194 C30H27N5O4S 553.6 C1[C@H](N(CC2=CC=CC=C21)C(=O)C3=CC=CC(=C3)C(=N)N)C(=O)NC4=CC=C(C=C4)C5=CC=CC=C5S(=O)(=O)N IC50 = 180000 nM Poor binder T45299 Tissue-type plasminogen activator BV45PY (S)-2-(1-(3-(6-Chloronaphthalen-2-ylsulfonyl)-2-hydroxypropanoyl)piperidin-4-yl)-5-methyl-1H-imidazo[1,5-c]imidazol-3(2H)-one Investigative 46196561 C24H25ClN4O5S 517 CC1=NC=C2N1C(=O)N(C2)C3CCN(CC3)C(=O)[C@@H](CS(=O)(=O)C4=CC5=C(C=C4)C=C(C=C5)Cl)O Ki ~ 60000 nM Poor binder T45299 Tissue-type plasminogen activator BW27LG (2S)-N-[(4-Aminocyclohexyl)methyl]-1-(3,3-dicyclohexylpropanoyl)pyrrolidine-2-carboxamide;hydrochloride Investigative 45261772 C27H48ClN3O2 482.1 C1CCC(CC1)C(CC(=O)N2CCC[C@H]2C(=O)NCC3CCC(CC3)N)C4CCCCC4.Cl Ki = 84000 nM Poor binder T45299 Tissue-type plasminogen activator BW6SN2 Substituted glycine deriv. 24 Investigative 16657882 C16H20ClN5O4S 413.9 CC(C)(C)[C@H](C(=O)O)NS(=O)(=O)C1=CC2=C(C=C1)C(=CN=C2N=C(N)N)Cl Ki ~ 100000 nM Poor binder T45299 Tissue-type plasminogen activator BW9UX0 (20S)-20-Benzyl-25-chloro-1,4,13,18,21,23-hexazatricyclo[20.3.1.06,11]hexacosa-6,8,10,22,24-pentaene-3,26-dione Investigative 135528485 C27H33ClN6O2 509 C1CCNCC2=CC=CC=C2CNC(=O)CN3C(=CN=C(C3=O)N[C@H](CNC1)CC4=CC=CC=C4)Cl Ki = 165000 nM Poor binder T45299 Tissue-type plasminogen activator BWIE23 Substituted glycine deriv. 25 Investigative 16657950 C20H20ClN5O4S 461.9 C[C@@H](C(=O)O)N(CC1=CC=CC=C1)S(=O)(=O)C2=CC3=C(C=C2)C(=CN=C3N=C(N)N)Cl Ki ~ 100000 nM Poor binder T45299 Tissue-type plasminogen activator BX4HS5 2-Carboxyindole-based inhibitor 8 Investigative 10412365 C24H25ClN4O2S 469 CCN1CCC(CC1)NC(=O)C2=CC3=CC=CC=C3N2CC4=NOC(=C4)C5=CC=C(S5)Cl Ki ~ 100000 nM Poor binder T45299 Tissue-type plasminogen activator BX9G8U N-[1-(Piperidinocarbonyl)-2-[4-(diaminomethyl)phenyl]ethyl]-2-[(2-naphthylsulfonyl)amino]acetamide Investigative 44367382 C27H33N5O4S 523.6 C1CCN(CC1)C(=O)C(CC2=CC=C(C=C2)C(N)N)NC(=O)CNS(=O)(=O)C3=CC4=CC=CC=C4C=C3 Ki = 70000 nM Poor binder T45299 Tissue-type plasminogen activator BY1V3F Substituted glycine deriv. 27 Investigative 9930716 C15H16ClN5O4S 397.8 C1CC(C1)(C(=O)O)NS(=O)(=O)C2=CC3=C(C=C2)C(=CN=C3N=C(N)N)Cl Ki ~ 100000 nM Poor binder T45299 Tissue-type plasminogen activator BY24QF N-(7-Bromo-isoquinolin-1-yl)-guanidine Investigative 44339277 C10H9BrN4 265.11 C1=CC(=CC2=C1C=CN=C2N=C(N)N)Br Ki = 95100 nM Poor binder T45299 Tissue-type plasminogen activator BY95OX 2-[3-[(E)-4-Methoxystyryl]-5-chloro-2-pyridinyl]guanidine Investigative 44298507 C15H15ClN4O 302.76 COC1=CC=C(C=C1)/C=C/C2=C(N=CC(=C2)Cl)N=C(N)N Ki = 60100 nM Poor binder T45299 Tissue-type plasminogen activator BZ56DU (2S)-N-Cyclopentyl-N-methyl-5-[4-(methylamino)phenyl]-2-(5,6,7,8-tetrahydronaphthalen-2-ylsulfonylamino)pent-4-ynamide Investigative 10345602 C28H35N3O3S 493.7 CNC1=CC=C(C=C1)C#CC[C@@H](C(=O)N(C)C2CCCC2)NS(=O)(=O)C3=CC4=C(CCCC4)C=C3 Ki = 200000 nM Poor binder T45299 Tissue-type plasminogen activator BZ7W8H Substituted glycine deriv. 18 Investigative 16658745 C19H18ClN5O4S 447.9 C1=CC=C(C=C1)CN(CC(=O)O)S(=O)(=O)C2=CC3=C(C=C2)C(=CN=C3N=C(N)N)Cl Ki ~ 100000 nM Poor binder T45299 Tissue-type plasminogen activator BZSH38 N-(4-Guanidino-phenyl)-2-hydroxy-5-nitro-benzamide Investigative 44303721 C14H13N5O4 315.28 C1=CC(=CC=C1NC(=O)C2=C(C=CC(=C2)[N+](=O)[O-])O)N=C(N)N Ki ~ 95000 nM Poor binder T45299 Tissue-type plasminogen activator D06CJP 4-chloro-1-guanidino-7-isoquinolinesulphonamide Investigative 16658353 C10H10ClN5O2S 299.74 C1=CC2=C(C=C1S(=O)(=O)N)C(=NC=C2Cl)N=C(N)N Ki ~ 100000 nM Poor binder T45299 Tissue-type plasminogen activator D0A8WP 6-(N-Phenylcarbamyl)-2-Naphthalenecarboxamidine Investigative 447732 C18H15N3O 289.3 C1=CC=C(C=C1)NC(=O)C2=CC3=C(C=C2)C=C(C=C3)C(=N)N IC50 = 125000 nM Poor binder