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Assay Detail

CHEMBL652744

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

Binding
Ability to inhibit [3H]WB-4101 binding to alpha-1 adrenergic receptor was determined in rat
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Adrenergic receptor alpha-1 (CHEMBL1907610)
Type PROTEIN FAMILY
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 8 6.88 9.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL58792 FLUANISONE 2.0 1 9.06
CHEMBL58377 1 8.05
CHEMBL54 HALOPERIDOL 4.0 1 7.51
CHEMBL418140 1 7.24
CHEMBL62499 1 6.60
CHEMBL278044 1 5.96
CHEMBL59186 1 5.80
CHEMBL267044 LEVOSULPIRIDE 2.0 1 4.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL58792 FLUANISONE Ki = 0.87 nM 9.06
CHEMBL58377 Ki = 9.0 nM 8.05
CHEMBL54 HALOPERIDOL Ki = 31.0 nM 7.51
CHEMBL418140 Ki = 57.0 nM 7.24
CHEMBL62499 Ki = 250.0 nM 6.60
CHEMBL278044 Ki = 1100.0 nM 5.96
CHEMBL59186 Ki = 1600.0 nM 5.80
CHEMBL267044 LEVOSULPIRIDE Ki = 15000.0 nM 4.82