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Assay Detail

CHEMBL964504

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

Binding
Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cannabinoid receptor 1 (CHEMBL218)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Exploring the substituent effects on a novel series of C1'-dimethyl-aryl Delta8-tetrahydrocannabinol analogs.
Krishnamurthy M, Gurley S, Moore BM.
Bioorg Med Chem (2008) 16 : 6489 -6500
PubMed 18524604 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 8.20 8.97

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL519575 1 8.97
CHEMBL487464 1 8.80
CHEMBL471122 1 8.75
CHEMBL471297 1 8.73
CHEMBL471295 1 8.60
CHEMBL471366 1 8.56
CHEMBL521366 1 8.55
CHEMBL512511 1 8.50
CHEMBL487463 1 8.30
CHEMBL512531 1 8.28
CHEMBL472115 1 8.03
CHEMBL471296 1 7.96
CHEMBL119592 1 7.91
CHEMBL471367 1 7.86
CHEMBL471988 1 7.73
CHEMBL267227 DELTA-8-TETRAHYDROCANNABINOL 2.0 1 7.54
CHEMBL512343 1 7.46
CHEMBL471123 1 7.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL519575 Ki = 1.08 nM 8.97
CHEMBL487464 Ki = 1.59 nM 8.80
CHEMBL471122 Ki = 1.77 nM 8.75
CHEMBL471297 Ki = 1.85 nM 8.73
CHEMBL471295 Ki = 2.53 nM 8.60
CHEMBL471366 Ki = 2.72 nM 8.56
CHEMBL521366 Ki = 2.8 nM 8.55
CHEMBL512511 Ki = 3.13 nM 8.50
CHEMBL487463 Ki = 5.03 nM 8.30
CHEMBL512531 Ki = 5.26 nM 8.28
CHEMBL472115 Ki = 9.25 nM 8.03
CHEMBL471296 Ki = 11.0 nM 7.96
CHEMBL119592 Ki = 12.3 nM 7.91
CHEMBL471367 Ki = 13.7 nM 7.86
CHEMBL471988 Ki = 18.8 nM 7.73
CHEMBL267227 DELTA-8-TETRAHYDROCANNABINOL Ki = 28.5 nM 7.54
CHEMBL512343 Ki = 34.4 nM 7.46
CHEMBL471123 Ki = 76.1 nM 7.12