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Assay Detail

CHEMBL4426136

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

Binding
Displacement of [3H]-CP55940 from human CB1 receptor expressed in HEK293 EBNA cell membranes after 90 mins by liquid scintillation counting method
44
Total Activities
44
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

Chromenopyrazole, a Versatile Cannabinoid Scaffold with in Vivo Activity in a Model of Multiple Sclerosis.
Morales P, Gómez-Cañas M, Navarro G, Hurst DP, Carrillo-Salinas FJ, Lagartera L, Pazos R, Goya P, Reggio PH, Guaza C, Franco R, Fernández-Ruiz J, Jagerovic N.
J Med Chem (2016) 59 : 6753 -6771
PubMed 27309150 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 44 6.59 8.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4441538 1 8.35
CHEMBL4527391 1 8.28
CHEMBL111 RIMONABANT 4.0 1 8.14
CHEMBL4467761 1 7.85
CHEMBL4585657 1 7.81
CHEMBL4463214 1 7.73
CHEMBL4441649 1 7.72
CHEMBL4465748 1 7.65
CHEMBL4472364 1 7.54
CHEMBL188 WIN-552122 1 7.34
CHEMBL4581919 1 7.26
CHEMBL4557358 1 7.19
CHEMBL4591232 1 6.66
CHEMBL4577623 1 6.57
CHEMBL4588694 1 6.48
CHEMBL4441832 1 6.35
CHEMBL4483721 1 6.29
CHEMBL4554620 1 6.21
CHEMBL4438938 1 6.18
CHEMBL4435812 1 6.17
CHEMBL4563803 1 6.15
CHEMBL4475298 1 5.96
CHEMBL4474156 1 5.94
CHEMBL4553217 1 5.88
CHEMBL4574497 1 5.83
CHEMBL4443489 1 5.79
CHEMBL4450138 1 5.77
CHEMBL4437352 1 5.63
CHEMBL4448412 1 5.53
CHEMBL4563152 1 5.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4441538 Ki = 4.5 nM 8.35
CHEMBL4527391 Ki = 5.2 nM 8.28
CHEMBL111 RIMONABANT Ki = 7.3 nM 8.14
CHEMBL4467761 Ki = 14.2 nM 7.85
CHEMBL4585657 Ki = 15.4 nM 7.81
CHEMBL4463214 Ki = 18.6 nM 7.73
CHEMBL4441649 Ki = 19.1 nM 7.72
CHEMBL4465748 Ki = 22.4 nM 7.65
CHEMBL4472364 Ki = 28.5 nM 7.54
CHEMBL188 WIN-552122 Ki = 45.6 nM 7.34
CHEMBL4581919 Ki = 54.4 nM 7.26
CHEMBL4557358 Ki = 64.8 nM 7.19
CHEMBL4591232 Ki = 218.1 nM 6.66
CHEMBL4577623 Ki = 272.0 nM 6.57
CHEMBL4588694 Ki = 332.6 nM 6.48
CHEMBL4441832 Ki = 450.4 nM 6.35
CHEMBL4483721 Ki = 514.0 nM 6.29
CHEMBL4554620 Ki = 613.7 nM 6.21
CHEMBL4438938 Ki = 657.0 nM 6.18
CHEMBL4435812 Ki = 671.3 nM 6.17
CHEMBL4563803 Ki = 702.4 nM 6.15
CHEMBL4475298 Ki = 1086.0 nM 5.96
CHEMBL4474156 Ki = 1140.0 nM 5.94
CHEMBL4553217 Ki = 1331.0 nM 5.88
CHEMBL4574497 Ki = 1482.0 nM 5.83
CHEMBL4443489 Ki = 1613.0 nM 5.79
CHEMBL4450138 Ki = 1693.0 nM 5.77
CHEMBL4437352 Ki = 2324.0 nM 5.63
CHEMBL4448412 Ki = 2930.0 nM 5.53
CHEMBL4563152 Ki = 4159.0 nM 5.38
CHEMBL4451471 Ki = 5040.0 nM 5.30
CHEMBL4483043 Ki = 6512.0 nM 5.19
CHEMBL4529850 Ki = 6440.0 nM 5.19
CHEMBL4444725 Ki > 40000.0 nM -
CHEMBL4474930 Ki > 40000.0 nM -
CHEMBL4562832 Ki > 40000.0 nM -
CHEMBL4469015 Ki > 10000.0 nM -
CHEMBL4443532 Ki > 40000.0 nM -
CHEMBL4467161 Ki > 40000.0 nM -
CHEMBL4537285 Ki > 40000.0 nM -
CHEMBL4555137 Ki > 40000.0 nM -
CHEMBL4448335 Ki > 40000.0 nM -
CHEMBL4525232 Ki > 40000.0 nM -
CHEMBL4458641 Ki > 40000.0 nM -