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Assay Detail

CHEMBL675709

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

Binding
Displacement of [3H]- spiperone radioligand binding at the dopamine binding site of rat caudate
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Dopamine receptor (CHEMBL2093868)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Synthesis and receptor binding studies relevant to the neuroleptic activities of some 1-methyl-4-piperidylidene-9-substituted-pyrrolo[2,1-b][3]benzazepine derivatives.
Remy DC, Britcher SF, King SW, Anderson PS, Hunt CA, Randall WC, Bélanger P, Atkinson JG, Girard Y, Rooney CS, Fuentes JJ, Totaro JA, Robinson JL, Risley EA, Williams M.
J Med Chem (1983) 26 : 974 -980
PubMed 6134835 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 7.35 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1255588 1 9.70
CHEMBL267930 SPIPERONE 2.0 1 8.70
CHEMBL368578 1 8.15
CHEMBL415761 1 7.96
CHEMBL175508 1 7.96
CHEMBL368475 1 7.92
CHEMBL424967 1 7.77
CHEMBL368357 1 7.70
CHEMBL178376 1 7.57
CHEMBL176365 1 7.50
CHEMBL516 CYPROHEPTADINE 4.0 1 7.20
CHEMBL175154 1 6.94
CHEMBL368413 1 6.68
CHEMBL174649 1 4.36
CHEMBL442783 1 4.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1255588 Ki = 0.2 nM 9.70
CHEMBL267930 SPIPERONE Ki = 2.0 nM 8.70
CHEMBL368578 Ki = 7.0 nM 8.15
CHEMBL415761 Ki = 11.0 nM 7.96
CHEMBL175508 Ki = 11.1 nM 7.96
CHEMBL368475 Ki = 12.0 nM 7.92
CHEMBL424967 Ki = 17.0 nM 7.77
CHEMBL368357 Ki = 20.0 nM 7.70
CHEMBL178376 Ki = 27.0 nM 7.57
CHEMBL176365 Ki = 32.0 nM 7.50
CHEMBL516 CYPROHEPTADINE Ki = 63.0 nM 7.20
CHEMBL175154 Ki = 114.0 nM 6.94
CHEMBL368413 Ki = 210.0 nM 6.68
CHEMBL174649 Ki = 43500.0 nM 4.36
CHEMBL442783 Ki = 80000.0 nM 4.10