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Assay Detail

CHEMBL679940

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

Binding
Binding affinity towards Dopamine receptor D2 in rat striatal tissue by [3H]spiperone displacement.
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

D(2) dopamine receptor (CHEMBL339)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Dopamine receptor binding properties of some 2,3,4,5-tetrahydro-1H-3-benzazepine-7-ols with non-aromatic substituents in the 5-position
Chang WK, Peters M, Fevig VP, Kozlowski JA, Zhou G, Lowe DB, Guzik H, McQuade RD, Duffy R, Coffin VL, Berger JG
Bioorg Med Chem Lett (1992) 2 : 399 -402
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 5.97 6.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL340006 1 6.58
CHEMBL334728 1 6.55
CHEMBL130328 1 6.24
CHEMBL127843 1 6.20
CHEMBL62 SCH-23390 1 6.12
CHEMBL130851 1 5.94
CHEMBL336532 1 5.92
CHEMBL340855 1 5.81
CHEMBL131054 1 5.80
CHEMBL128649 1 5.75
CHEMBL422796 1 5.75
CHEMBL339342 1 5.69
CHEMBL336610 1 5.65
CHEMBL338237 1 5.57
CHEMBL128917 1 -
CHEMBL334650 1 -
CHEMBL340324 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL340006 Ki = 265.0 nM 6.58
CHEMBL334728 Ki = 284.0 nM 6.55
CHEMBL130328 Ki = 581.0 nM 6.24
CHEMBL127843 Ki = 626.0 nM 6.20
CHEMBL62 SCH-23390 Ki = 760.0 nM 6.12
CHEMBL130851 Ki = 1160.0 nM 5.94
CHEMBL336532 Ki = 1190.0 nM 5.92
CHEMBL340855 Ki = 1540.0 nM 5.81
CHEMBL131054 Ki = 1600.0 nM 5.80
CHEMBL128649 Ki = 1800.0 nM 5.75
CHEMBL422796 Ki = 1780.0 nM 5.75
CHEMBL339342 Ki = 2050.0 nM 5.69
CHEMBL336610 Ki = 2250.0 nM 5.65
CHEMBL338237 Ki = 2710.0 nM 5.57
CHEMBL128917 Ki > 10000.0 nM -
CHEMBL334650 Ki > 10000.0 nM -
CHEMBL340324 Ki > 100000.0 nM -