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Assay Detail

CHEMBL827435

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

Functional
Binding affinity for cannabinoid receptor 2 was determined by using [35S]GTP-gamma-S, as radioligand
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Triaryl bis-sulfones as a new class of cannabinoid CB2 receptor inhibitors: identification of a lead and initial SAR studies.
Lavey BJ, Kozlowski JA, Hipkin RW, Gonsiorek W, Lundell DJ, Piwinski JJ, Narula S, Lunn CA.
Bioorg Med Chem Lett (2005) 15 : 783 -786
PubMed 15664857 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 7.20 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL181843 1 9.52
CHEMBL180465 1 9.40
CHEMBL181288 1 9.00
CHEMBL180748 1 8.21
CHEMBL359712 1 8.11
CHEMBL180450 1 7.80
CHEMBL181677 1 7.54
CHEMBL182151 1 7.51
CHEMBL180788 1 7.41
CHEMBL360306 1 7.39
CHEMBL181675 1 6.80
CHEMBL362822 1 6.78
CHEMBL180963 1 6.62
CHEMBL360697 1 6.54
CHEMBL361957 1 6.38
CHEMBL180196 1 6.30
CHEMBL361218 1 6.30
CHEMBL426962 1 6.10
CHEMBL179888 1 5.95
CHEMBL181868 1 5.90
CHEMBL362480 1 5.61

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL181843 Ki = 0.3 nM 9.52
CHEMBL180465 Ki = 0.4 nM 9.40
CHEMBL181288 Ki = 1.0 nM 9.00
CHEMBL180748 Ki = 6.2 nM 8.21
CHEMBL359712 Ki = 7.7 nM 8.11
CHEMBL180450 Ki = 15.7 nM 7.80
CHEMBL181677 Ki = 29.0 nM 7.54
CHEMBL182151 Ki = 31.0 nM 7.51
CHEMBL180788 Ki = 38.6 nM 7.41
CHEMBL360306 Ki = 41.0 nM 7.39
CHEMBL181675 Ki = 160.0 nM 6.80
CHEMBL362822 Ki = 167.0 nM 6.78
CHEMBL180963 Ki = 239.0 nM 6.62
CHEMBL360697 Ki = 289.0 nM 6.54
CHEMBL361957 Ki = 412.0 nM 6.38
CHEMBL180196 Ki = 495.0 nM 6.30
CHEMBL361218 Ki = 495.0 nM 6.30
CHEMBL426962 Ki = 802.0 nM 6.10
CHEMBL179888 Ki = 1136.0 nM 5.95
CHEMBL181868 Ki = 1258.0 nM 5.90
CHEMBL362480 Ki = 2476.0 nM 5.61