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Assay Detail

CHEMBL1670561

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [3H]CP 55940 from human CB2 receptor in cell free system
ChEMBL ↗
119
Total Activities
119
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cannabinoid receptor 2 (CHEMBL253) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Three-dimensional quantitative structure-selectivity relationships analysis guided rational design of a highly selective ligand for the cannabinoid receptor 2.
Brogi S, Corelli F, Di Marzo V, Ligresti A, Mugnaini C, Pasquini S, Tafi A.
Eur J Med Chem (2011) 46 : 547 -555
PubMed 21183257 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 119 7.99 10.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL216276 — — 1 10.40
CHEMBL411631 — — 1 10.00
CHEMBL271839 — — 1 9.70
CHEMBL108085 — — 1 9.70
CHEMBL252949 — — 1 9.66
CHEMBL411244 — — 1 9.40
CHEMBL564901 — — 1 9.22
CHEMBL559612 CP-55940 — 1 9.22
CHEMBL1668519 — — 1 9.19
CHEMBL270125 — — 1 9.15
CHEMBL1215942 — — 1 9.15
CHEMBL270546 — — 1 9.05
CHEMBL19847 — — 1 9.05
CHEMBL519575 — — 1 9.04
CHEMBL117033 — — 1 8.98
CHEMBL1668505 — — 1 8.92
CHEMBL272876 — — 1 8.89
CHEMBL271824 — — 1 8.89
CHEMBL120669 — — 1 8.89
CHEMBL188 WIN-552122 — 1 8.89
CHEMBL599882 — — 1 8.80
CHEMBL272203 — — 1 8.77
CHEMBL596579 — — 1 8.77
CHEMBL1215941 — — 1 8.64
CHEMBL1668517 — — 1 8.62
CHEMBL1668514 — — 1 8.57
CHEMBL599071 — — 1 8.57
CHEMBL306529 — — 1 8.54
CHEMBL1668396 — — 1 8.52
CHEMBL570690 — — 1 8.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL216276 — Ki = 0.04 nM 10.40
CHEMBL411631 — Ki = 0.1 nM 10.00
CHEMBL108085 — Ki = 0.2 nM 9.70
CHEMBL271839 — Ki = 0.2 nM 9.70
CHEMBL252949 — Ki = 0.22 nM 9.66
CHEMBL411244 — Ki = 0.4 nM 9.40
CHEMBL564901 — Ki = 0.6 nM 9.22
CHEMBL559612 CP-55940 Ki = 0.6 nM 9.22
CHEMBL1668519 — Ki = 0.64 nM 9.19
CHEMBL270125 — Ki = 0.7 nM 9.15
CHEMBL1215942 — Ki = 0.7 nM 9.15
CHEMBL270546 — Ki = 0.9 nM 9.05
CHEMBL19847 — Ki = 0.9 nM 9.05
CHEMBL519575 — Ki = 0.91 nM 9.04
CHEMBL117033 — Ki = 1.05 nM 8.98
CHEMBL1668505 — Ki = 1.2 nM 8.92
CHEMBL188 WIN-552122 Ki = 1.3 nM 8.89
CHEMBL272876 — Ki = 1.3 nM 8.89
CHEMBL120669 — Ki = 1.3 nM 8.89
CHEMBL271824 — Ki = 1.3 nM 8.89
CHEMBL599882 — Ki = 1.6 nM 8.80
CHEMBL596579 — Ki = 1.7 nM 8.77
CHEMBL272203 — Ki = 1.7 nM 8.77
CHEMBL1215941 — Ki = 2.3 nM 8.64
CHEMBL1668517 — Ki = 2.4 nM 8.62
CHEMBL1668514 — Ki = 2.7 nM 8.57
CHEMBL599071 — Ki = 2.7 nM 8.57
CHEMBL306529 — Ki = 2.9 nM 8.54
CHEMBL1668396 — Ki = 3.0 nM 8.52
CHEMBL570690 — Ki = 3.1 nM 8.51
CHEMBL571777 — Ki = 3.3 nM 8.48
CHEMBL371214 — Ki = 3.4 nM 8.47
CHEMBL524456 — Ki = 3.4 nM 8.47
CHEMBL1668504 — Ki = 3.5 nM 8.46
CHEMBL523577 — Ki = 3.8 nM 8.42
CHEMBL1668512 — Ki = 3.9 nM 8.41
CHEMBL205888 — Ki = 3.9 nM 8.41
CHEMBL1215918 — Ki = 4.2 nM 8.38
CHEMBL1668508 — Ki = 4.266 nM 8.37
CHEMBL262865 — Ki = 4.4 nM 8.36
CHEMBL1216000 — Ki = 4.4 nM 8.36
CHEMBL272882 — Ki = 4.6 nM 8.34
CHEMBL201571 — Ki = 4.7 nM 8.33
CHEMBL1668518 — Ki = 4.9 nM 8.31
CHEMBL474897 — Ki = 5.2 nM 8.28
CHEMBL381689 SR-144528 Ki = 5.4 nM 8.27
CHEMBL303479 — Ki = 5.4 nM 8.27
CHEMBL1668506 — Ki = 5.7 nM 8.24
CHEMBL502276 — Ki = 6.3 nM 8.20
CHEMBL1668395 — Ki = 6.5 nM 8.19