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Assay Detail

CHEMBL659689

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Binding
Binding affinity towards cannabinoid receptor 1 from rat forebrain membranes in the presence of phenylmethanesulfonylfluoride (PMSF) using 0.8 nM [3H]CP-55940 as radioligand
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Forebrain
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Cannabinoid receptor 1 (CHEMBL3571)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Novel analogues of arachidonylethanolamide (anandamide): affinities for the CB1 and CB2 cannabinoid receptors and metabolic stability.
Lin S, Khanolkar AD, Fan P, Goutopoulos A, Qin C, Papahadjis D, Makriyannis A.
J Med Chem (1998) 41 : 5353 -5361
PubMed 9876105 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 6.83 8.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL151167 1 8.28
CHEMBL274016 1 8.00
CHEMBL359165 1 7.97
CHEMBL120526 METHANANDAMIDE 1 7.75
CHEMBL151864 1 7.59
CHEMBL74909 1 7.57
CHEMBL330974 1 7.45
CHEMBL151504 1 7.44
CHEMBL150942 1 7.29
CHEMBL15848 ANANDAMIDE 1 7.21
CHEMBL359278 1 7.13
CHEMBL151496 1 7.08
CHEMBL421967 1 7.04
CHEMBL150849 1 6.94
CHEMBL346659 1 6.89
CHEMBL149691 1 6.82
CHEMBL151862 1 6.54
CHEMBL348466 1 6.51
CHEMBL151717 1 6.38
CHEMBL149859 LINOLEOYLETHANOLAMIDE 1 5.00
CHEMBL151084 1 4.72
CHEMBL280065 OLEOYLETHANOLAMIDE 1 4.70
CHEMBL356213 1 4.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL151167 Ki = 5.29 nM 8.28
CHEMBL274016 Ki = 9.91 nM 8.00
CHEMBL359165 Ki = 10.8 nM 7.97
CHEMBL120526 METHANANDAMIDE Ki = 17.9 nM 7.75
CHEMBL151864 Ki = 25.6 nM 7.59
CHEMBL74909 Ki = 26.7 nM 7.57
CHEMBL330974 Ki = 35.6 nM 7.45
CHEMBL151504 Ki = 36.2 nM 7.44
CHEMBL150942 Ki = 51.2 nM 7.29
CHEMBL15848 ANANDAMIDE Ki = 61.0 nM 7.21
CHEMBL359278 Ki = 73.6 nM 7.13
CHEMBL151496 Ki = 83.2 nM 7.08
CHEMBL421967 Ki = 90.2 nM 7.04
CHEMBL150849 Ki = 115.0 nM 6.94
CHEMBL346659 Ki = 130.0 nM 6.89
CHEMBL149691 Ki = 151.0 nM 6.82
CHEMBL151862 Ki = 287.0 nM 6.54
CHEMBL348466 Ki = 309.0 nM 6.51
CHEMBL151717 Ki = 421.0 nM 6.38
CHEMBL149859 LINOLEOYLETHANOLAMIDE Ki = 10000.0 nM 5.00
CHEMBL151084 Ki = 19000.0 nM 4.72
CHEMBL280065 OLEOYLETHANOLAMIDE Ki = 20000.0 nM 4.70
CHEMBL356213 Ki = 21000.0 nM 4.68