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Assay Detail

CHEMBL658880

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Binding
Concentration of compound required to inhibit 50% of [3H]WIN-55212 binding to Cannabinoid receptor 1 in rat cerebellum membranes.
ChEMBL ↗
62
Total Activities
61
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Aminoalkylindoles: structure-activity relationships of novel cannabinoid mimetics.
Eissenstat MA, Bell MR, D'Ambra TE, Alexander EJ, Daum SJ, Ackerman JH, Gruett MD, Kumar V, Estep KG, Olefirowicz EM.
J Med Chem (1995) 38 : 3094 -3105
PubMed 7636873 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 62 6.99 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL81473 — — 1 8.85
CHEMBL80214 — — 1 8.55
CHEMBL309605 — — 1 8.47
CHEMBL82361 — — 1 8.46
CHEMBL465 DRONABINOL 4.0 1 8.24
CHEMBL309763 — — 1 8.23
CHEMBL78359 — — 1 8.16
CHEMBL13078 — — 1 8.11
CHEMBL78940 — — 1 8.00
CHEMBL78713 — — 1 8.00
CHEMBL78415 — — 1 8.00
CHEMBL78994 — — 1 7.96
CHEMBL104841 — — 1 7.89
CHEMBL81683 — — 1 7.82
CHEMBL78375 — — 1 7.75
CHEMBL274833 — — 1 7.72
CHEMBL80337 — — 1 7.62
CHEMBL107106 — — 2 7.48
CHEMBL78308 — — 1 7.46
CHEMBL311645 — — 1 7.43
CHEMBL311560 — — 1 7.42
CHEMBL323501 — — 1 7.37
CHEMBL312057 — — 1 7.26
CHEMBL307073 — — 1 7.23
CHEMBL79204 — — 1 7.23
CHEMBL78627 — — 1 7.16
CHEMBL107136 — — 1 7.15
CHEMBL78815 — — 1 6.96
CHEMBL319464 — — 1 6.91
CHEMBL78763 — — 1 6.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL81473 — IC50 = 1.4 nM 8.85
CHEMBL80214 — IC50 = 2.8 nM 8.55
CHEMBL309605 — IC50 = 3.4 nM 8.47
CHEMBL82361 — IC50 = 3.5 nM 8.46
CHEMBL465 DRONABINOL IC50 = 5.8 nM 8.24
CHEMBL309763 — IC50 = 5.9 nM 8.23
CHEMBL78359 — IC50 = 6.9 nM 8.16
CHEMBL13078 — IC50 = 7.8 nM 8.11
CHEMBL78415 — IC50 = 10.0 nM 8.00
CHEMBL78940 — IC50 = 10.0 nM 8.00
CHEMBL78713 — IC50 = 10.0 nM 8.00
CHEMBL78994 — IC50 = 11.0 nM 7.96
CHEMBL104841 — IC50 = 13.0 nM 7.89
CHEMBL81683 — IC50 = 15.0 nM 7.82
CHEMBL78375 — IC50 = 18.0 nM 7.75
CHEMBL274833 — IC50 = 19.0 nM 7.72
CHEMBL80337 — IC50 = 24.0 nM 7.62
CHEMBL107106 — IC50 = 33.0 nM 7.48
CHEMBL78308 — IC50 = 35.0 nM 7.46
CHEMBL311645 — IC50 = 37.0 nM 7.43
CHEMBL311560 — IC50 = 38.0 nM 7.42
CHEMBL323501 — IC50 = 43.0 nM 7.37
CHEMBL312057 — IC50 = 55.0 nM 7.26
CHEMBL79204 — IC50 = 59.0 nM 7.23
CHEMBL307073 — IC50 = 59.0 nM 7.23
CHEMBL78627 — IC50 = 70.0 nM 7.16
CHEMBL107136 — IC50 = 71.0 nM 7.15
CHEMBL78815 — IC50 = 110.0 nM 6.96
CHEMBL107106 — IC50 = 114.0 nM 6.94
CHEMBL319464 — IC50 = 124.0 nM 6.91
CHEMBL78763 — IC50 = 128.0 nM 6.89
CHEMBL311667 — IC50 = 138.0 nM 6.86
CHEMBL78995 — IC50 = 140.0 nM 6.85
CHEMBL431862 — IC50 = 150.0 nM 6.82
CHEMBL310995 — IC50 = 177.0 nM 6.75
CHEMBL311328 — IC50 = 186.0 nM 6.73
CHEMBL80938 — IC50 = 274.0 nM 6.56
CHEMBL77445 — IC50 = 283.0 nM 6.55
CHEMBL309756 — IC50 = 304.0 nM 6.52
CHEMBL78752 — IC50 = 306.0 nM 6.51
CHEMBL311065 — IC50 = 331.0 nM 6.48
CHEMBL81911 — IC50 = 357.0 nM 6.45
CHEMBL312259 — IC50 = 373.0 nM 6.43
CHEMBL80984 — IC50 = 384.0 nM 6.42
CHEMBL273606 — IC50 = 390.0 nM 6.41
CHEMBL431589 — IC50 = 416.0 nM 6.38
CHEMBL78992 — IC50 = 491.0 nM 6.31
CHEMBL309700 — IC50 = 499.0 nM 6.30
CHEMBL310741 — IC50 = 515.0 nM 6.29
CHEMBL78701 — IC50 = 571.0 nM 6.24