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Assay Detail

CHEMBL672000

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

Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

D(1A) dopamine receptor (CHEMBL265)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists.
Balle T, Perregaard J, Ramirez MT, Larsen AK, Søby KK, Liljefors T, Andersen K.
J Med Chem (2003) 46 : 265 -283
PubMed 12519065 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 6.01 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL12713 SERTINDOLE 4.0 1 7.92
CHEMBL54 HALOPERIDOL 4.0 1 7.54
CHEMBL318901 1 5.80
CHEMBL95175 1 5.75
CHEMBL97242 1 5.58
CHEMBL317333 1 5.52
CHEMBL327527 1 5.39
CHEMBL313424 1 5.35
CHEMBL97333 1 5.25
CHEMBL2 PRAZOSIN 4.0 1 -
CHEMBL319352 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL12713 SERTINDOLE Ki = 12.0 nM 7.92
CHEMBL54 HALOPERIDOL Ki = 29.0 nM 7.54
CHEMBL318901 Ki = 1600.0 nM 5.80
CHEMBL95175 Ki = 1800.0 nM 5.75
CHEMBL97242 Ki = 2600.0 nM 5.58
CHEMBL317333 Ki = 3000.0 nM 5.52
CHEMBL327527 Ki = 4100.0 nM 5.39
CHEMBL313424 Ki = 4500.0 nM 5.35
CHEMBL97333 Ki = 5600.0 nM 5.25
CHEMBL2 PRAZOSIN Ki > 5600.0 nM -
CHEMBL319352 Ki > 100.0 nM -