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Assay Detail

CHEMBL643614

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

Binding
Binding affinity for Alpha-1 adrenergic receptor measured by displacing [3H]prazosin from rat cortical membranes
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Alpha-1A adrenergic receptor (CHEMBL319)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Pyrimido[5,4-b]indole derivatives. 1. A new class of potent and selective alpha 1 adrenoceptor ligands.
Russo F, Romeo G, Guccione S, De Blasi A.
J Med Chem (1991) 34 : 1850 -1854
PubMed 1648138 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 9.02 9.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL301707 1 9.68
CHEMBL54716 1 9.49
CHEMBL57163 1 9.28
CHEMBL51963 1 8.74
CHEMBL55528 1 7.89
CHEMBL52473 1 -
CHEMBL57398 1 -
CHEMBL55338 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL301707 Ki = 0.21 nM 9.68
CHEMBL54716 Ki = 0.32 nM 9.49
CHEMBL57163 Ki = 0.53 nM 9.28
CHEMBL51963 Ki = 1.8 nM 8.74
CHEMBL55528 Ki = 13.0 nM 7.89
CHEMBL52473 Ki > 5000.0 nM -
CHEMBL57398 Ki > 100000.0 nM -
CHEMBL55338 Ki >= 10000.0 nM -