Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T76685 | ||||
Target Name | Cannabinoid receptor 1 (CB1) | ||||
Type of Target |
Successful |
||||
Drug Potency against Target | Drug Info | Ki = 5.6 nM | [42] | ||
Marinol | Drug Info | Ki = 35.3 nM | [41] | ||
Conatumumab | Drug Info | Ki = 1.3 nM | [7] | ||
Drug Info | Ki = 700 nM | [26] | |||
Drug Info | Ki = 700 nM | [26] | |||
(1R,2R)-N-Arachidonoylcyclopropanolamide | Drug Info | Ki = 11 nM | [26] | ||
(1R,2S)-N-Arachidonoylcyclopropanolamide | Drug Info | Ki = 20 nM | [26] | ||
(1R,2S)-N-Oleoylcyclopropanolamide | Drug Info | Ki = 820 nM | [26] | ||
(1S,2S)-N-Arachidonoylcyclopropanolamide | Drug Info | Ki = 28 nM | [26] | ||
(1S,2S)-N-Oleoylcyclopropanolamide | Drug Info | Ki = 1400 nM | [26] | ||
(2R)-N-(6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDIN-4-YL)-2-HYDROXYPROPANAMIDE (ENANTIOMERIC MIX) | Drug Info | IC50 = 16 nM | [34] | ||
(2R)-N-(7'-(2-CHLOROPHENYL)-6'-(4-CHLOROPHENYL)-3',4'-DIHYDROSPIRO[CYCLOHEXANE-1,2'-PYRANO[2,3-B]PYRIDINE]-4'-YL)-2-HYDROXYPROPANAMIDE (ENANTIOMERIC MIX) | Drug Info | IC50 = 2 nM | [34] | ||
(2S)-N-(7'-(2-CHLOROPHENYL)-6'-(4-CHLOROPHENYL)-3',4'-DIHYDROSPIRO[CYCLOHEXANE-1,2'-PYRANO[2,3-B]PYRIDINE]-4'-YL)-2-HYDROXYPROPANAMIDE (ENANTIOMERIC MIX) | Drug Info | IC50 = 13 nM | [34] | ||
(4-benzhydrylpiperazin-1-yl)(cyclohexyl)methanone | Drug Info | Ki = 164 nM | [31] | ||
(E)-N-(3,5-dimethoxyphenethyl)undec-2-enamide | Drug Info | Ki = 2800 nM | [3] | ||
(E)-N-(4-methoxyphenethyl)undec-2-enamide | Drug Info | Ki = 2400 nM | [3] | ||
(E)-N-(4-methoxyphenyl)undec-2-enamide | Drug Info | Ki = 4900 nM | [3] | ||
1,3,5-triphenylimidazolidine-2,4-dione | Drug Info | Ki = 6296 nM | [6] | ||
1,3,5-tris(4-chlorophenyl)imidazolidine-2,4-dione | Drug Info | Ki = 2618 nM | [6] | ||
1,4-dihydroindeno[1,2-c]-pyrazole | Drug Info | Ki = 2050 nM | [4] | ||
1,5-bis(4-chlorophenyl)-1H-1,2,3-triazole | Drug Info | Ki = 6900 nM | [23] | ||
1-(4-CHLOROPHENYL)-2-(2,4-DICHLOROPHENYL)-5-(METHYLSULFINYL)-N-(PIPERIDIN-1-YL)-1H-IMIDAZOLE-4-CARBOXAMIDE (ENANTIOMERIC MIX) | Drug Info | Ki = 49 nM | [32] | ||
1-(bis(4-bromophenyl)methyl)-3-phenylurea | Drug Info | Ki = 2900 nM | [5] | ||
1-(bis(4-chlorophenyl)methyl)-3-phenylurea | Drug Info | Ki = 7050 nM | [5] | ||
1-[bis(4-bromophenyl)methyl]-3-phenylthiourea | Drug Info | Ki = 1800 nM | [5] | ||
1-[bis(4-chlorophenyl)methyl]-3-(4-chlorophenyl)- | Drug Info | Ki = 1100 nM | [5] | ||
1-[bis(4-chlorophenyl)methyl]-3-phenylthiourea | Drug Info | Ki = 2900 nM | [5] | ||
1-[bis(4-iodophenyl)methyl]-3-(4-bromophenyl)urea | Drug Info | Ki = 750 nM | [5] | ||
2'-amino-4-(1,1-dimethyl-heptyl)-biphenyl-2-ol | Drug Info | Ki = 5.2 nM | [10] | ||
2-Benzylbenzo[f]chromen-3-one | Drug Info | Ki = 4190 nM | [25] | ||
3'-amino-4-(1,1-dimethyl-heptyl)-biphenyl-2-ol | Drug Info | Ki = 15 nM | [10] | ||
3-Benzyl-5-isopropyl-8-methylchromen-2-one | Drug Info | Ki = 2760 nM | [25] | ||
3-Benzyl-5-methoxy-7-methylchromen-2-one | Drug Info | Ki = 3460 nM | [25] | ||
3-Benzyl-5-methoxychromen-2-one | Drug Info | Ki = 19100 nM | [25] | ||
4'-amino-4-(1,1-dimethyl-heptyl)-biphenyl-2-ol | Drug Info | Ki = 320 nM | [10] | ||
4-(1,1-dimethyl-heptyl)-2'-methoxy-biphenyl-2-ol | Drug Info | Ki = 1.7 nM | [10] | ||
4-(1,1-dimethyl-heptyl)-3'-methoxy-biphenyl-2-ol | Drug Info | Ki = 91 nM | [10] | ||
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one | Drug Info | Ki < 1000 nM | [37] | ||
4-benzhydryl-N-butylpiperazine-1-carboxamide | Drug Info | Ki = 239 nM | [31] | ||
4-benzhydryl-N-cyclohexylpiperazine-1-carboxamide | Drug Info | Ki = 52 nM | [31] | ||
4-cyanophenyl ethyl dodecylphosphonate | Drug Info | IC50 = 4 nM | [19] | ||
5-(1,1-dimethyl-heptyl)-2-pyridin-3-yl-phenol | Drug Info | Ki = 23 nM | [10] | ||
5-Biphenyl-4-ylmethyl-2-isobutyl-2H-tetrazole | Drug Info | Ki = 1600 nM | [15] | ||
5-Methoxy-3-(2-methoxybenzyl)-2H-chromen-2-one | Drug Info | Ki = 9570 nM | [25] | ||
6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDINE-4-CARBOXAMIDE (ENANTIOMERIC MIX) | Drug Info | IC50 = 220 nM | [34] | ||
6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-N-((R)-1-HYDROXYETHYL)-1,2,2-TRIMETHYL-1,2,3,4-TETRAHYDRO-1,8-NAPHTHYRIDINE-4-CARBOXAMIDE (ENANTIOMERIC MIX) | Drug Info | IC50 = 29 nM | [34] | ||
6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-N-(1-HYDROXY-2-METHYLPROPAN-2-YL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDINE-4-CARBOXAMIDE (ENANTIOMERIC MIX) | Drug Info | IC50 = 150 nM | [34] | ||
6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-N-(HYDROXYMETHYL)-1,2,2-TRIMETHYL-1,2,3,4-TETRAHYDRO-1,8-NAPHTHYRIDINE-4-CARBOXAMIDE (ENANTIOMERIC MIX) | Drug Info | IC50 = 76 nM | [34] | ||
A-796260 | Drug Info | Ki = 945 nM | [29] | ||
AM-1241 | Drug Info | Ki = 1269 nM | [29] | ||
AM-1710 | Drug Info | Ki = 360 nM | [14] | ||
AM-1714 | Drug Info | Ki = 400 nM | [14] | ||
AM-1715 | Drug Info | Ki = 5.4 nM | [14] | ||
AM-281 | Drug Info | Ki = 12.4 nM | [25] | ||
AM-404 | Drug Info | Ki = 1760 nM | [40] | ||
AM-411 | Drug Info | Ki = 6.8 nM | [35] | ||
AM-4768 | Drug Info | Ki = 2.6 nM | [14] | ||
AM-630 | Drug Info | Ki = 840 nM | [13] | ||
Chlorphrifos oxon | Drug Info | IC50 = 3 nM | [19] | ||
Cis-N-oleoylcyclopropanolamide | Drug Info | Ki = 600 nM | [26] | ||
CP-4497 | Drug Info | Ki = 9.54 nM | [36] | ||
DELTA 8-TETRAHYDROCANNOBINOL | Drug Info | Ki = 47.6 nM | [20] | ||
Dodecane-1-sulfonyl fluoride | Drug Info | IC50 = 7 nM | [19] | ||
Isopropyl 4-nitrophenyl dodecylphosphonate | Drug Info | IC50 = 12 nM | [19] | ||
Isopropyl dodecylfluorophosphonate | Drug Info | IC50 = 2 nM | [16] | ||
JWH-120 | Drug Info | Ki = 1054 nM | [24] | ||
JWH-133 | Drug Info | Ki = 677 nM | [39] | ||
JWH-145 | Drug Info | Ki = 14 nM | [9] | ||
JWH-146 | Drug Info | Ki = 21 nM | [9] | ||
JWH-147 | Drug Info | Ki = 11 nM | [9] | ||
JWH-150 | Drug Info | Ki = 60 nM | [9] | ||
JWH-156 | Drug Info | Ki = 404 nM | [9] | ||
JWH-229 | Drug Info | Ki = 3134 nM | [24] | ||
JWH-243 | Drug Info | Ki = 285 nM | [9] | ||
JWH-244 | Drug Info | Ki = 130 nM | [9] | ||
JWH-245 | Drug Info | Ki = 276 nM | [9] | ||
JWH-246 | Drug Info | Ki = 70 nM | [9] | ||
JWH-268 | Drug Info | Ki = 1379 nM | [24] | ||
JWH-292 | Drug Info | Ki = 29 nM | [9] | ||
JWH-293 | Drug Info | Ki = 100 nM | [9] | ||
JWH-297 | Drug Info | Ki = 8626 nM | [12] | ||
JWH-307 | Drug Info | Ki = 7.7 nM | [9] | ||
JWH-308 | Drug Info | Ki = 41 nM | [9] | ||
JWH-309 | Drug Info | Ki = 41 nM | [9] | ||
JWH-324 | Drug Info | Ki = 2954 nM | [36] | ||
JWH-325 | Drug Info | Ki = 579 nM | [12] | ||
JWH-337 | Drug Info | Ki = 547 nM | [12] | ||
JWH-344 | Drug Info | Ki = 308 nM | [12] | ||
JWH-345 | Drug Info | Ki = 266 nM | [12] | ||
JWH-346 | Drug Info | Ki = 67 nM | [9] | ||
JWH-347 | Drug Info | Ki = 333 nM | [9] | ||
JWH-348 | Drug Info | Ki = 218 nM | [9] | ||
JWH-363 | Drug Info | Ki = 245 nM | [9] | ||
JWH-364 | Drug Info | Ki = 34 nM | [9] | ||
JWH-365 | Drug Info | Ki = 17 nM | [9] | ||
JWH-366 | Drug Info | Ki = 191 nM | [9] | ||
JWH-367 | Drug Info | Ki = 53 nM | [9] | ||
JWH-368 | Drug Info | Ki = 16 nM | [9] | ||
JWH-369 | Drug Info | Ki = 7.9 nM | [9] | ||
JWH-370 | Drug Info | Ki = 5.6 nM | [9] | ||
JWH-371 | Drug Info | Ki = 42 nM | [9] | ||
JWH-372 | Drug Info | Ki = 77 nM | [9] | ||
JWH-373 | Drug Info | Ki = 60 nM | [9] | ||
JWH-385 | Drug Info | Ki = 566 nM | [12] | ||
JWH-392 | Drug Info | Ki = 3795 nM | [12] | ||
JWH-401 | Drug Info | Ki = 1707 nM | [12] | ||
JWH-402 | Drug Info | Ki = 749 nM | [12] | ||
JWH-403 | Drug Info | Ki = 2113 nM | [12] | ||
JWH-404 | Drug Info | Ki = 786 nM | [12] | ||
JWH-405 | Drug Info | Ki = 193 nM | [12] | ||
JWH-406 | Drug Info | Ki = 1028 nM | [12] | ||
JWH-407 | Drug Info | Ki = 1731 nM | [12] | ||
JWH-440 | Drug Info | Ki = 4414 nM | [36] | ||
JWH-442 | Drug Info | Ki = 4123 nM | [36] | ||
KM-233-M | Drug Info | Ki = 5.26 nM | [17] | ||
Methyl icosylphosphonofluoridate | Drug Info | IC50 = 20 nM | [19] | ||
N-(1-adamantyl)-N'-propylsulfamide | Drug Info | Ki = 4229 nM | [28] | ||
N-(1H-indazol-5-yl)icosa-5,8,11,14-tetraenamide | Drug Info | Ki = 300 nM | [22] | ||
N-(2,4-dimethoxyphenethyl)docos-13-enamide | Drug Info | Ki = 3700 nM | [3] | ||
N-(2,4-dimethoxyphenethyl)oleamide | Drug Info | Ki = 600 nM | [3] | ||
N-(2-adamantyl)-N'-propylsulfamide | Drug Info | Ki = 6670 nM | [28] | ||
N-(2-chloroethyl)icosa-5,8,11,14-tetraenamide | Drug Info | Ki = 5.3 nM | [13] | ||
N-(3,3-Diphenyl)propyl-2,2-diphenylacetamide | Drug Info | Ki = 58 nM | [18] | ||
N-(3,3-Diphenyl)propyl-2-phenylacetamide | Drug Info | Ki = 560 nM | [18] | ||
N-(3,5-dimethoxyphenethyl)docos-13-enamide | Drug Info | Ki = 5400 nM | [3] | ||
N-(3,5-dimethoxyphenethyl)oleamide | Drug Info | Ki = 1000 nM | [3] | ||
N-(3-Phenyl)propyl-2,2-diphenylacetamide | Drug Info | Ki = 3400 nM | [18] | ||
N-(3-Phenyl)propyl-2-(4-bromophenylacetamide) | Drug Info | Ki = 1900 nM | [18] | ||
N-(4-hydroxybenzyl)icosa-5,8,11,14-tetraenamide | Drug Info | Ki = 200 nM | [22] | ||
N-(4-methoxybenzyl)oleamide | Drug Info | Ki = 600 nM | [3] | ||
N-(4-methoxyphenethyl)oleamide | Drug Info | Ki = 300 nM | [3] | ||
N-(4-methoxyphenyl)oleamide | Drug Info | Ki = 1500 nM | [3] | ||
N-(4-morpholinophenyl)docos-13-enamide | Drug Info | Ki = 6400 nM | [3] | ||
N-(6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDIN-4-YL)-2-HYDROXYACETAMIDE (ENANTIOMERIC MIX) | Drug Info | IC50 = 670 nM | [34] | ||
N-(6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDIN-4-YL)-3-HYDROXY-2,2-DIMETHYLPROPANAMIDE (ENANTIOMERIC MIX) | Drug Info | IC50 = 34 nM | [34] | ||
N-(6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDIN-4-YL)-3-HYDROXYPROPANAMIDE (ENANTIOMERIC MIX) | Drug Info | IC50 = 14 nM | [34] | ||
N-(7'-(2-CHLOROPHENYL)-6'-(4-CHLOROPHENYL)-3',4'-DIHYDROSPIRO[CYCLOHEXANE-1,2'-PYRANO[2,3-B]PYRIDINE]-4'-YL)-2-HYDROXY-2-METHYLPROPANAMIDE (ENANTIOMERIC MIX) | Drug Info | IC50 = 18 nM | [34] | ||
N-(7-(2-CHLOROPHENYL)-6-(4-CHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDIN-4-YL)-2-HYDROXYACETAMIDE (ENANTIOMERIC MIX) | Drug Info | IC50 = 360 nM | [34] | ||
N-(cis-9-cis-12-octadecadienyl)sulfamide | Drug Info | Ki = 6406 nM | [28] | ||
N-arachidonoyl-N-(2-hydroxyethyl)hydroxylamine | Drug Info | Ki = 3900 nM | [8] | ||
N-arachidonoyl-O-(2-hydroxyethyl)hydroxylamine | Drug Info | Ki = 470 nM | [8] | ||
N-ethyl-5,6-dip-tolylpyrazine-2-carboxamide | Drug Info | Ki = 2381 nM | [11] | ||
N-isopentyl-5,6-dip-tolylpyrazine-2-carboxamide | Drug Info | Ki = 178 nM | [11] | ||
N-isopropyl-5,6-dip-tolylpyrazine-2-carboxamide | Drug Info | Ki = 656 nM | [11] | ||
N-methyl-5,6-dip-tolylpyrazine-2-carboxamide | Drug Info | Ki = 3848 nM | [11] | ||
N-octadecyl-N'-propylsulfamide | Drug Info | Ki = 9102 nM | [28] | ||
N-oleoylethanolamide | Drug Info | Ki = 1100 nM | [26] | ||
N-phenyl-5,6-dip-tolylpyrazine-2-carboxamide | Drug Info | Ki = 509 nM | [11] | ||
N-[6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDINE-4-YL]-4,4,4-TRIFLUORO-3-HYDROXYBUTANAMIDE (DIASTEREOMERIC MIX) | Drug Info | IC50 = 1.7 nM | [33] | ||
NABILONE | Drug Info | Ki = 2.2 nM | [38] | ||
NAPHTHYRIDINONE | Drug Info | IC50 = 7.5 nM | [34] | ||
O-arachidonoyl-N-(2-hydroxyethyl)hydroxylamine | Drug Info | Ki = 3500 nM | [8] | ||
Octane-1-sulfonyl fluoride | Drug Info | IC50 = 1300 nM | [19] | ||
Orlistat | Drug Info | Ki = 2500 nM | [21] | ||
PARAOXON | Drug Info | IC50 = 1200 nM | [19] | ||
PRAVADOLINE | Drug Info | IC50 = 3155 nM | |||
Rac-cis-N-arachidonoylcyclopropanolamide | Drug Info | Ki = 27 nM | [26] | ||
Rac-trans-N-oleoylcyclopropanolamide | Drug Info | Ki = 570 nM | [26] | ||
SCH-356036 | Drug Info | Ki = 3538 nM | [30] | ||
SEMIPLENAMIDE A | Drug Info | Ki = 19500 nM | [1] | ||
SEMIPLENAMIDE B | Drug Info | Ki = 18700 nM | [1] | ||
Semiplenamide G | Drug Info | Ki = 17900 nM | [1] | ||
SR-147778 | Drug Info | Ki = 3.5 nM | [2] | ||
VER-156084 | Drug Info | Ki = 560 nM | [27] | ||
VER-156084 | Drug Info | Ki < 10 nM | [27] | ||
VER-156085 | Drug Info | Ki < 10 nM | [27] | ||
WIN-55212-2 | Drug Info | Ki = 6.06 nM | [25] | ||
[3H]CP55940 | Drug Info | Ki = 1.24 nM | [25] | ||
{[(9Z)-octadec-9-en-1-yl]sulfamoyl}amine | Drug Info | Ki = 1890 nM | [28] | ||
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