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Assay Detail

CHEMBL659697

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Binding
In vitro binding affinity was determined against rat brain Cannabinoid receptor 1
53
Total Activities
51
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Structural requirements for binding of anandamide-type compounds to the brain cannabinoid receptor.
Sheskin T, Hanus L, Slager J, Vogel Z, Mechoulam R.
J Med Chem (1997) 40 : 659 -667
PubMed 9057852 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 53 7.08 8.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL160350 1 8.16
CHEMBL423602 1 8.14
CHEMBL158649 1 8.13
CHEMBL160975 1 8.08
CHEMBL429055 1 7.93
CHEMBL16424 1 7.87
CHEMBL423382 1 7.59
CHEMBL277297 1 7.52
CHEMBL2110161 1 7.51
CHEMBL158468 1 7.49
CHEMBL15873 1 7.47
CHEMBL321585 1 7.46
CHEMBL15848 ANANDAMIDE 1 7.41
CHEMBL2110295 1 7.33
CHEMBL121229 1 7.27
CHEMBL15755 1 7.22
CHEMBL75591 1 7.07
CHEMBL150942 1 6.86
CHEMBL2110160 1 6.81
CHEMBL161521 1 6.79
CHEMBL162244 1 6.79
CHEMBL2110296 1 6.72
CHEMBL158956 1 6.72
CHEMBL15566 1 6.63
CHEMBL359278 1 6.62
CHEMBL161520 1 6.49
CHEMBL151862 1 6.42
CHEMBL159181 1 6.35
CHEMBL160717 1 6.30
CHEMBL158544 1 6.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL160350 Ki = 6.9 nM 8.16
CHEMBL423602 Ki = 7.2 nM 8.14
CHEMBL158649 Ki = 7.4 nM 8.13
CHEMBL160975 Ki = 8.4 nM 8.08
CHEMBL429055 Ki = 11.7 nM 7.93
CHEMBL16424 Ki = 13.6 nM 7.87
CHEMBL423382 Ki = 25.5 nM 7.59
CHEMBL277297 Ki = 29.9 nM 7.52
CHEMBL2110161 Ki = 31.1 nM 7.51
CHEMBL158468 Ki = 32.5 nM 7.49
CHEMBL15873 Ki = 34.0 nM 7.47
CHEMBL321585 Ki = 34.4 nM 7.46
CHEMBL15848 ANANDAMIDE Ki = 39.2 nM 7.41
CHEMBL2110295 Ki = 46.6 nM 7.33
CHEMBL121229 Ki = 53.4 nM 7.27
CHEMBL15755 Ki = 60.0 nM 7.22
CHEMBL75591 Ki = 85.2 nM 7.07
CHEMBL150942 Ki = 138.6 nM 6.86
CHEMBL2110160 Ki = 153.9 nM 6.81
CHEMBL162244 Ki = 161.8 nM 6.79
CHEMBL161521 Ki = 162.3 nM 6.79
CHEMBL158956 Ki = 190.8 nM 6.72
CHEMBL2110296 Ki = 191.4 nM 6.72
CHEMBL15566 Ki = 235.7 nM 6.63
CHEMBL359278 Ki = 239.9 nM 6.62
CHEMBL161520 Ki = 324.1 nM 6.49
CHEMBL151862 Ki = 377.2 nM 6.42
CHEMBL159181 Ki = 446.7 nM 6.35
CHEMBL160717 Ki = 497.4 nM 6.30
CHEMBL158544 Ki = 575.1 nM 6.24
CHEMBL121316 Ki = 1500.0 nM 5.82
CHEMBL149859 LINOLEOYLETHANOLAMIDE Ki = 4600.0 nM 5.34
CHEMBL160313 Ki - nM -
CHEMBL15567 Ki > 1000.0 nM -
CHEMBL15812 Ki > 1000.0 nM -
CHEMBL158367 Ki > 10000.0 nM -
CHEMBL277123 Ki > 1000.0 nM -
CHEMBL161343 ARACHIDONOYL GLYCINE Ki > 10000.0 nM -
CHEMBL15948 Ki > 10000.0 nM -
CHEMBL161596 Ki > 10000.0 nM -
CHEMBL417675 PALMIDROL Ki - nM -
CHEMBL158880 Ki > 1000.0 nM -
CHEMBL158277 Ki > 1000.0 nM -
CHEMBL160351 Ki - nM -
CHEMBL15150 ARACHIDONAMIDE Ki > 1000.0 nM -
CHEMBL160854 Ki > 10000.0 nM -
CHEMBL160854 Ki > 10000.0 nM -
CHEMBL149859 LINOLEOYLETHANOLAMIDE Ki > 25000.0 nM -
CHEMBL347615 Ki > 1000.0 nM -
CHEMBL159221 Ki > 10000.0 nM -