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Assay Detail

CHEMBL672377

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

Binding
Ability to inhibit the [3H]spiperone binding to striatum Dopamine receptor D2 was determined in rat
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Striatum
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 1.
van Wijngaarden I, Kruse CG, van Hes R, van der Heyden JA, Tulp MT.
J Med Chem (1987) 30 : 2099 -2104
PubMed 2889830 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 7.72 9.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL418140 1 9.04
CHEMBL54 HALOPERIDOL 4.0 1 8.85
CHEMBL58792 FLUANISONE 2.0 1 8.54
CHEMBL58377 1 8.30
CHEMBL60648 1 8.14
CHEMBL278044 1 8.03
CHEMBL277631 1 7.54
CHEMBL267044 LEVOSULPIRIDE 2.0 1 7.41
CHEMBL65107 1 6.82
CHEMBL62499 1 6.32
CHEMBL59186 1 5.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL418140 Ki = 0.91 nM 9.04
CHEMBL54 HALOPERIDOL Ki = 1.4 nM 8.85
CHEMBL58792 FLUANISONE Ki = 2.9 nM 8.54
CHEMBL58377 Ki = 5.0 nM 8.30
CHEMBL60648 Ki = 7.3 nM 8.14
CHEMBL278044 Ki = 9.3 nM 8.03
CHEMBL277631 Ki = 29.0 nM 7.54
CHEMBL267044 LEVOSULPIRIDE Ki = 39.0 nM 7.41
CHEMBL65107 Ki = 150.0 nM 6.82
CHEMBL62499 Ki = 480.0 nM 6.32
CHEMBL59186 Ki = 1100.0 nM 5.96