Target Validation Information
Target ID T76685
Target Name Cannabinoid receptor 1
Target Type
Successful
Drug Potency against Target AM-1241 Drug Info Ki = 1269 nM [530525]
4-benzhydryl-N-cyclohexylpiperazine-1-carboxamide Drug Info Ki = 52 nM [530617]
4-benzhydryl-N-butylpiperazine-1-carboxamide Drug Info Ki = 239 nM [530617]
NABILONE Drug Info Ki = 2.2 nM [531196]
JWH-344 Drug Info Ki = 308 nM [529084]
JWH-385 Drug Info Ki = 566 nM [529084]
WIN-55212-2 Drug Info Ki = 6.06 nM [530009]
JWH-308 Drug Info Ki = 41 nM [528355]
JWH-367 Drug Info Ki = 53 nM [528355]
JWH-229 Drug Info Ki = 3134 nM [529920]
JWH-404 Drug Info Ki = 786 nM [529084]
JWH-373 Drug Info Ki = 60 nM [528355]
JWH-309 Drug Info Ki = 41 nM [528355]
JWH-337 Drug Info Ki = 547 nM [529084]
JWH-365 Drug Info Ki = 17 nM [528355]
A-796260 Drug Info Ki = 945 nM [530525]
JWH-145 Drug Info Ki = 14 nM [528355]
JWH-297 Drug Info Ki = 8626 nM [529084]
JWH-372 Drug Info Ki = 77 nM [528355]
JWH-345 Drug Info Ki = 266 nM [529084]
JWH-366 Drug Info Ki = 191 nM [528355]
JWH-325 Drug Info Ki = 579 nM [529084]
JWH-363 Drug Info Ki = 245 nM [528355]
1,3,5-tris(4-chlorophenyl)imidazolidine-2,4-dione Drug Info Ki = 2618 nM [527995]
N-(2,4-dimethoxyphenethyl)oleamide Drug Info Ki = 600 nM [527788]
JWH-150 Drug Info Ki = 60 nM [528355]
AM-1714 Drug Info Ki = 400 nM [529170]
JWH-370 Drug Info Ki = 5.6 nM [528355]
JWH-407 Drug Info Ki = 1731 nM [529084]
JWH-440 Drug Info Ki = 4414 nM [531027]
JWH-292 Drug Info Ki = 29 nM [528355]
JWH-243 Drug Info Ki = 285 nM [528355]
AM-1710 Drug Info Ki = 360 nM [529170]
JWH-346 Drug Info Ki = 67 nM [528355]
(1R,2S)-N-Oleoylcyclopropanolamide Drug Info Ki = 820 nM [530070]
Rac-cis-N-arachidonoylcyclopropanolamide Drug Info Ki = 27 nM [530070]
N-(2,4-dimethoxyphenethyl)docos-13-enamide Drug Info Ki = 3700 nM [527788]
O-arachidonoyl-N-(2-hydroxyethyl)hydroxylamine Drug Info Ki = 3500 nM [528112]
OLEOYLETHANOLAMIDE Drug Info Ki = 1100 nM [530070]
N-arachidonoyl-O-(2-hydroxyethyl)hydroxylamine Drug Info Ki = 470 nM [528112]
N-(3,5-dimethoxyphenethyl)docos-13-enamide Drug Info Ki = 5400 nM [527788]
(1R,2R)-N-Oleoylcyclopropanolamide Drug Info Ki = 700 nM [530070]
3-Benzyl-5-methoxy-7-methylchromen-2-one Drug Info Ki = 3460 nM [530009]
N-(3,3-Diphenyl)propyl-2,2-diphenylacetamide Drug Info Ki = 58 nM [529563]
CP-55940 Drug Info Ki = 1.24 nM [530009]
Isopropyl dodecylfluorophosphonate Drug Info IC50 = 2 nM [529440]
N-(4-methoxyphenethyl)oleamide Drug Info Ki = 300 nM [527788]
N-(2-chloroethyl)icosa-5,8,11,14-tetraenamide Drug Info Ki = 5.3 nM [529106]
3'-amino-4-(1,1-dimethyl-heptyl)-biphenyl-2-ol Drug Info Ki = 15 nM [528844]
N-isopropyl-5,6-dip-tolylpyrazine-2-carboxamide Drug Info Ki = 656 nM [528851]
N-(1H-indazol-5-yl)icosa-5,8,11,14-tetraenamide Drug Info Ki = 300 nM [529838]
(4-benzhydrylpiperazin-1-yl)(cyclohexyl)methanone Drug Info Ki = 164 nM [530617]
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 [530929]
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 [530929]
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 [530929]
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 [530929]
NAPHTHYRIDINONE Drug Info IC50 = 7.5 nM [530929]
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 [530929]
VER-156084 Drug Info Ki = 560 nM [530200]
N-(4-hydroxybenzyl)icosa-5,8,11,14-tetraenamide Drug Info Ki = 200 nM [529838]
2-Benzylbenzo[f]chromen-3-one Drug Info Ki = 4190 nM [530009]
Rimonabant Drug Info Ki = 5.6 nM [552786]
1-(4-CHLOROPHENYL)-2-(2,4-DICHLOROPHENYL)-5-(METHYLSULFINYL)-N-(PIPERIDIN-1-YL)-1H-IMIDAZOLE-4-CARBOXAMIDE (ENANTIOMERIC MIX) Drug Info Ki = 49 nM [530827]
PARAOXON Drug Info IC50 = 1200 nM [529659]
AM-630 Drug Info Ki = 840 nM [529106]
1-(bis(4-bromophenyl)methyl)-3-phenylurea Drug Info Ki = 2900 nM [527861]
(1S,2S)-N-Oleoylcyclopropanolamide Drug Info Ki = 1400 nM [530070]
1,4-dihydroindeno[1,2-c]-pyrazole Drug Info Ki = 2050 nM [527858]
AM-4768 Drug Info Ki = 2.6 nM [529170]
JWH-406 Drug Info Ki = 1028 nM [529084]
JWH-147 Drug Info Ki = 11 nM [528355]
JWH-401 Drug Info Ki = 1707 nM [529084]
JWH-307 Drug Info Ki = 7.7 nM [528355]
JWH-244 Drug Info Ki = 130 nM [528355]
JWH-403 Drug Info Ki = 2113 nM [529084]
JWH-368 Drug Info Ki = 16 nM [528355]
CP-4497 Drug Info Ki = 9.54 nM [531027]
JWH-364 Drug Info Ki = 34 nM [528355]
JWH-348 Drug Info Ki = 218 nM [528355]
JWH-245 Drug Info Ki = 276 nM [528355]
JWH-246 Drug Info Ki = 70 nM [528355]
JWH-392 Drug Info Ki = 3795 nM [529084]
JWH-268 Drug Info Ki = 1379 nM [529920]
JWH-402 Drug Info Ki = 749 nM [529084]
JWH-405 Drug Info Ki = 193 nM [529084]
JWH-156 Drug Info Ki = 404 nM [528355]
JWH-293 Drug Info Ki = 100 nM [528355]
JWH-371 Drug Info Ki = 42 nM [528355]
JWH-324 Drug Info Ki = 2954 nM [531027]
JWH-369 Drug Info Ki = 7.9 nM [528355]
JWH-146 Drug Info Ki = 21 nM [528355]
Dodecane-1-sulfonyl fluoride Drug Info IC50 = 7 nM [529659]
VER-156084 Drug Info Ki < 10 nM [530200]
1-(bis(4-chlorophenyl)methyl)-3-phenylurea Drug Info Ki = 7050 nM [527861]
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 [530929]
(1R,2S)-N-Arachidonoylcyclopropanolamide Drug Info Ki = 20 nM [530070]
Methyl icosylphosphonofluoridate Drug Info IC50 = 20 nM [529659]
N-(3,5-dimethoxyphenethyl)oleamide Drug Info Ki = 1000 nM [527788]
(E)-N-(4-methoxyphenethyl)undec-2-enamide Drug Info Ki = 2400 nM [527788]
N-(4-morpholinophenyl)docos-13-enamide Drug Info Ki = 6400 nM [527788]
3-Benzyl-5-isopropyl-8-methylchromen-2-one Drug Info Ki = 2760 nM [530009]
Chlorphrifos oxon Drug Info IC50 = 3 nM [529659]
1-[bis(4-iodophenyl)methyl]-3-(4-bromophenyl)urea Drug Info Ki = 750 nM [527861]
N-(cis-9-cis-12-octadecadienyl)sulfamide Drug Info Ki = 6406 nM [530389]
N-(4-methoxybenzyl)oleamide Drug Info Ki = 600 nM [527788]
Rac-trans-N-oleoylcyclopropanolamide Drug Info Ki = 570 nM [530070]
(1S,2R)-N-Oleoylcyclopropanolamide Drug Info Ki = 700 nM [530070]
Cis-N-oleoylcyclopropanolamide Drug Info Ki = 600 nM [530070]
(1R,2R)-N-Arachidonoylcyclopropanolamide Drug Info Ki = 11 nM [530070]
5-Methoxy-3-(2-methoxybenzyl)-2H-chromen-2-one Drug Info Ki = 9570 nM [530009]
N-(3-Phenyl)propyl-2,2-diphenylacetamide Drug Info Ki = 3400 nM [529563]
N-(2-adamantyl)-N'-propylsulfamide Drug Info Ki = 6670 nM [530389]
1-[bis(4-chlorophenyl)methyl]-3-(4-chlorophenyl)- Drug Info Ki = 1100 nM [527861]
N-(4-methoxyphenyl)oleamide Drug Info Ki = 1500 nM [527788]
1-[bis(4-chlorophenyl)methyl]-3-phenylthiourea Drug Info Ki = 2900 nM [527861]
2'-amino-4-(1,1-dimethyl-heptyl)-biphenyl-2-ol Drug Info Ki = 5.2 nM [528844]
N-arachidonoyl-N-(2-hydroxyethyl)hydroxylamine Drug Info Ki = 3900 nM [528112]
AM-281 Drug Info Ki = 12.4 nM [530009]
4-(1,1-dimethyl-heptyl)-2'-methoxy-biphenyl-2-ol Drug Info Ki = 1.7 nM [528844]
4-(1,1-dimethyl-heptyl)-3'-methoxy-biphenyl-2-ol Drug Info Ki = 91 nM [528844]
N-methyl-5,6-dip-tolylpyrazine-2-carboxamide Drug Info Ki = 3848 nM [528851]
N-phenyl-5,6-dip-tolylpyrazine-2-carboxamide Drug Info Ki = 509 nM [528851]
5-(1,1-dimethyl-heptyl)-2-pyridin-3-yl-phenol Drug Info Ki = 23 nM [528844]
1-[bis(4-bromophenyl)methyl]-3-phenylthiourea Drug Info Ki = 1800 nM [527861]
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 [530929]
(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 [530929]
(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 [530929]
N-(1-adamantyl)-N'-propylsulfamide Drug Info Ki = 4229 nM [530389]
{[(9Z)-octadec-9-en-1-yl]sulfamoyl}amine Drug Info Ki = 1890 nM [530389]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info Ki < 1000 nM [531079]
Isopropyl 4-nitrophenyl dodecylphosphonate Drug Info IC50 = 12 nM [529659]
4-cyanophenyl ethyl dodecylphosphonate Drug Info IC50 = 4 nM [529659]
3-Benzyl-5-methoxychromen-2-one Drug Info Ki = 19100 nM [530009]
TETRAHYDROLIPSTATIN Drug Info Ki = 2500 nM [529733]
1,5-bis(4-chlorophenyl)-1H-1,2,3-triazole Drug Info Ki = 6900 nM [529882]
JWH-133 Drug Info Ki = 677 nM [531214]
(E)-N-(4-methoxyphenyl)undec-2-enamide Drug Info Ki = 4900 nM [527788]
(1S,2S)-N-Arachidonoylcyclopropanolamide Drug Info Ki = 28 nM [530070]
1,3,5-triphenylimidazolidine-2,4-dione Drug Info Ki = 6296 nM [527995]
JWH-442 Drug Info Ki = 4123 nM [531027]
N-isopentyl-5,6-dip-tolylpyrazine-2-carboxamide Drug Info Ki = 178 nM [528851]
Octane-1-sulfonyl fluoride Drug Info IC50 = 1300 nM [529659]
AM-404 Drug Info Ki = 1760 nM [534262]
5-Biphenyl-4-ylmethyl-2-isobutyl-2H-tetrazole Drug Info Ki = 1600 nM [529434]
SCH-356036 Drug Info Ki = 3538 nM [530597]
N-(3-Phenyl)propyl-2-(4-bromophenylacetamide) Drug Info Ki = 1900 nM [529563]
SEMIPLENAMIDE A Drug Info Ki = 19500 nM [526859]
AZD1940 Drug Info Ki = 1.3 nM [528068]
(E)-N-(3,5-dimethoxyphenethyl)undec-2-enamide Drug Info Ki = 2800 nM [527788]
JWH-120 Drug Info Ki = 1054 nM [529920]
JWH-347 Drug Info Ki = 333 nM [528355]
(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 [530929]
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 [530929]
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 [530929]
Marinol Drug Info Ki = 35.3 nM [552785]
Semiplenamide G Drug Info Ki = 17900 nM [526859]
SEMIPLENAMIDE B Drug Info Ki = 18700 nM [526859]
KM-233-M Drug Info Ki = 5.26 nM [529515]
AM-411 Drug Info Ki = 6.8 nM [531004]
N-octadecyl-N'-propylsulfamide Drug Info Ki = 9102 nM [530389]
PRAVADOLINE Drug Info IC50 = 3155 nM
AM-1715 Drug Info Ki = 5.4 nM [529170]
SR-147778 Drug Info Ki = 3.5 nM [527671]
DELTA 8-TETRAHYDROCANNOBINOL Drug Info Ki = 47.6 nM [529727]
N-ethyl-5,6-dip-tolylpyrazine-2-carboxamide Drug Info Ki = 2381 nM [528851]
4'-amino-4-(1,1-dimethyl-heptyl)-biphenyl-2-ol Drug Info Ki = 320 nM [528844]
N-(3,3-Diphenyl)propyl-2-phenylacetamide Drug Info Ki = 560 nM [529563]
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 [530871]
VER-156085 Drug Info Ki < 10 nM [530200]
References
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Ref 530617Eur J Med Chem. 2010 Mar;45(3):1133-9. Epub 2009 Dec 16.Discovery of benzhydrylpiperazine derivatives as CB1 receptor inverse agonists via privileged structure-based approach.
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