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Assay Detail

CHEMBL1636583

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Binding
Selectivity index ratio of Ki for recombinant human CB2 to Ki for recombinant human CB1 receptor
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Synthesis and biological evaluation of new N-alkyl 1-aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamides as cannabinoid receptor ligands.
Silvestri R, Ligresti A, La Regina G, Piscitelli F, Gatti V, Lavecchia A, Brizzi A, Pasquini S, Allarà M, Fantini N, Carai MA, Bigogno C, Rozio MG, Sinisi R, Novellino E, Colombo G, Di Marzo V, Dondio G, Corelli F.
Eur J Med Chem (2010) 45 : 5878 -5886
PubMed 20943290 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 27 8.66 9.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1629731 1 9.96
CHEMBL1631297 1 9.89
CHEMBL1631294 1 9.80
CHEMBL1631298 1 9.21
CHEMBL1631292 1 9.00
CHEMBL1631289 1 8.94
CHEMBL1631165 1 8.92
CHEMBL1631300 1 8.89
CHEMBL1631295 1 8.82
CHEMBL1631290 1 8.81
CHEMBL1631301 1 8.74
CHEMBL1631291 1 8.68
CHEMBL1631293 1 8.66
CHEMBL1631162 1 8.60
CHEMBL1631160 1 8.57
CHEMBL1631168 1 8.56
CHEMBL1631161 1 8.54
CHEMBL1631164 1 8.51
CHEMBL1631299 1 8.45
CHEMBL1631167 1 8.43
CHEMBL1631163 1 8.36
CHEMBL1631166 1 8.17
CHEMBL1631296 1 8.11
CHEMBL1631169 1 8.07
CHEMBL285932 1 7.31
CHEMBL111 RIMONABANT 4.0 1 7.18
CHEMBL381689 SR-144528 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1629731 Ki = 0.11 nM 9.96
CHEMBL1631297 Ki = 0.13 nM 9.89
CHEMBL1631294 Ki = 0.16 nM 9.80
CHEMBL1631298 Ki = 0.62 nM 9.21
CHEMBL1631292 Ki = 0.99 nM 9.00
CHEMBL1631289 Ki = 1.15 nM 8.94
CHEMBL1631165 Ki = 1.21 nM 8.92
CHEMBL1631300 Ki = 1.29 nM 8.89
CHEMBL1631295 Ki = 1.51 nM 8.82
CHEMBL1631290 Ki = 1.56 nM 8.81
CHEMBL1631301 Ki = 1.8 nM 8.74
CHEMBL1631291 Ki = 2.11 nM 8.68
CHEMBL1631293 Ki = 2.18 nM 8.66
CHEMBL1631162 Ki = 2.54 nM 8.60
CHEMBL1631160 Ki = 2.71 nM 8.57
CHEMBL1631168 Ki = 2.72 nM 8.56
CHEMBL1631161 Ki = 2.91 nM 8.54
CHEMBL1631164 Ki = 3.09 nM 8.51
CHEMBL1631299 Ki = 3.56 nM 8.45
CHEMBL1631167 Ki = 3.73 nM 8.43
CHEMBL1631163 Ki = 4.38 nM 8.36
CHEMBL1631166 Ki = 6.73 nM 8.17
CHEMBL1631296 Ki = 7.69 nM 8.11
CHEMBL1631169 Ki = 8.59 nM 8.07
CHEMBL285932 Ki = 48.7 nM 7.31
CHEMBL111 RIMONABANT Ki = 65.83 nM 7.18
CHEMBL381689 SR-144528 Ki < 0.002 nM -