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Assay Detail

CHEMBL646107

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

Binding
Compound was tested for binding affinity utilizing cloned receptor binding assays by using [125 I]HEAT as radioligand to the human Alpha-1D adrenergic receptor
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Alpha-1D adrenergic receptor (CHEMBL223)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

4-Amino-2-[4-[1-(benzyloxycarbonyl)-2(S)- [[(1,1-dimethylethyl)amino]carbonyl]-piperazinyl]-6, 7-dimethoxyquinazoline (L-765,314): a potent and selective alpha1b adrenergic receptor antagonist.
Patane MA, Scott AL, Broten TP, Chang RS, Ransom RW, DiSalvo J, Forray C, Bock MG.
J Med Chem (1998) 41 : 1205 -1208
PubMed 9548811 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 7.81 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2 PRAZOSIN 4.0 1 9.70
CHEMBL19826 1 7.14
CHEMBL19376 1 6.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2 PRAZOSIN Ki = 0.2 nM 9.70
CHEMBL19826 Ki = 73.0 nM 7.14
CHEMBL19376 Ki = 250.0 nM 6.60