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Assay Detail

CHEMBL1670560

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

Binding
Displacement of [3H]CP 55940 from human CB1 receptor in cell free system
ChEMBL ↗
101
Total Activities
101
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 1 (CHEMBL218) ↗
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 101 6.58 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL108085 — — 1 9.30
CHEMBL559612 CP-55940 — 1 9.22
CHEMBL252949 — — 1 9.03
CHEMBL19847 — — 1 9.00
CHEMBL564901 — — 1 8.89
CHEMBL120669 — — 1 8.74
CHEMBL117033 — — 1 8.73
CHEMBL272203 — — 1 8.25
CHEMBL205888 — — 1 8.08
CHEMBL1668516 — — 1 8.08
CHEMBL306529 — — 1 8.02
CHEMBL381492 — — 1 7.93
CHEMBL519575 — — 1 7.91
CHEMBL188 WIN-552122 — 1 7.88
CHEMBL271824 — — 1 7.85
CHEMBL303479 — — 1 7.65
CHEMBL271839 — — 1 7.55
CHEMBL1668396 — — 1 7.55
CHEMBL261381 — — 1 7.55
CHEMBL270546 — — 1 7.48
CHEMBL201571 — — 1 7.38
CHEMBL1668395 — — 1 7.38
CHEMBL411631 — — 1 7.35
CHEMBL1354658 — — 1 7.32
CHEMBL1668505 — — 1 7.28
CHEMBL1668521 — — 1 7.02
CHEMBL1668512 — — 1 6.89
CHEMBL570907 — — 1 6.88
CHEMBL474897 — — 1 6.70
CHEMBL571777 — — 1 6.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL108085 — Ki = 0.5 nM 9.30
CHEMBL559612 CP-55940 Ki = 0.6 nM 9.22
CHEMBL252949 — Ki = 0.94 nM 9.03
CHEMBL19847 — Ki = 1.0 nM 9.00
CHEMBL564901 — Ki = 1.3 nM 8.89
CHEMBL120669 — Ki = 1.8 nM 8.74
CHEMBL117033 — Ki = 1.86 nM 8.73
CHEMBL272203 — Ki = 5.6 nM 8.25
CHEMBL205888 — Ki = 8.3 nM 8.08
CHEMBL1668516 — Ki = 8.4 nM 8.08
CHEMBL306529 — Ki = 9.5 nM 8.02
CHEMBL381492 — Ki = 11.7 nM 7.93
CHEMBL519575 — Ki = 12.3 nM 7.91
CHEMBL188 WIN-552122 Ki = 13.3 nM 7.88
CHEMBL271824 — Ki = 14.0 nM 7.85
CHEMBL303479 — Ki = 22.3 nM 7.65
CHEMBL271839 — Ki = 28.0 nM 7.55
CHEMBL1668396 — Ki = 28.0 nM 7.55
CHEMBL261381 — Ki = 28.0 nM 7.55
CHEMBL270546 — Ki = 33.0 nM 7.48
CHEMBL201571 — Ki = 42.0 nM 7.38
CHEMBL1668395 — Ki = 42.0 nM 7.38
CHEMBL411631 — Ki = 45.0 nM 7.35
CHEMBL1354658 — Ki = 48.3 nM 7.32
CHEMBL1668505 — Ki = 53.0 nM 7.28
CHEMBL1668521 — Ki = 95.0 nM 7.02
CHEMBL1668512 — Ki = 130.0 nM 6.89
CHEMBL570907 — Ki = 131.0 nM 6.88
CHEMBL474897 — Ki = 200.0 nM 6.70
CHEMBL571777 — Ki = 220.0 nM 6.66
CHEMBL411244 — Ki = 228.0 nM 6.64
CHEMBL272876 — Ki = 234.0 nM 6.63
CHEMBL1668519 — Ki = 270.0 nM 6.57
CHEMBL272882 — Ki = 280.0 nM 6.55
CHEMBL258242 — Ki = 310.0 nM 6.51
CHEMBL216276 — Ki = 363.0 nM 6.44
CHEMBL306764 — Ki = 383.0 nM 6.42
CHEMBL474896 — Ki = 390.0 nM 6.41
CHEMBL511150 — Ki = 470.0 nM 6.33
CHEMBL1668517 — Ki = 480.0 nM 6.32
CHEMBL1215898 — Ki = 510.0 nM 6.29
CHEMBL593434 — Ki = 560.0 nM 6.25
CHEMBL1668511 — Ki = 616.0 nM 6.21
CHEMBL524456 — Ki = 640.0 nM 6.19
CHEMBL1668514 — Ki = 650.0 nM 6.19
CHEMBL371214 — Ki = 677.0 nM 6.17
CHEMBL570690 — Ki = 710.0 nM 6.15
CHEMBL270125 — Ki = 780.0 nM 6.11
CHEMBL474692 — Ki = 790.0 nM 6.10
CHEMBL262865 — Ki = 845.0 nM 6.07