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Assay Detail

CHEMBL643869

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

Binding
Binding affinity against human Alpha-1b adrenergic receptor was evaluated by cloned receptor binding assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Alpha-1B adrenergic receptor (CHEMBL232)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Selective alpha-1a adrenergic receptor antagonists. Effects of pharmacophore regio- and stereochemistry on potency and selectivity.
Patane MA, DiPardo RM, Price RP, Chang RS, Ransom RW, O'Malley SS, Di Salvo J, Bock MG.
Bioorg Med Chem Lett (1998) 8 : 2495 -2500
PubMed 9873568 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 6.19 6.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL82267 1 6.77
CHEMBL8412 IPSAPIRONE 2.0 1 6.66
CHEMBL1169493 1 6.03
CHEMBL418926 1 5.85
CHEMBL79532 1 5.66
CHEMBL3349545 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL82267 Ki = 170.0 nM 6.77
CHEMBL8412 IPSAPIRONE Ki = 220.0 nM 6.66
CHEMBL1169493 Ki = 940.0 nM 6.03
CHEMBL418926 Ki = 1400.0 nM 5.85
CHEMBL79532 Ki = 2200.0 nM 5.66
CHEMBL3349545 Ki > 2000.0 nM -