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Assay Detail

CHEMBL3611840

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

Binding
Displacement of [3H]prazosin from alpha1B adrenoceptor in rat liver membranes
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Liver
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Alpha-1B adrenergic receptor (CHEMBL315)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Indolylpiperidine derivatives as potent and selective α1B adrenoceptor antagonists.
Hayashi R, Ohmori E, Moriwaki M, Kumagai H, Isogaya M.
Bioorg Med Chem Lett (2015) 25 : 3921 -3923
PubMed 26238322 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 8.09 9.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3609360 1 9.21
CHEMBL3609359 1 8.68
CHEMBL1188811 1 8.52
CHEMBL3609357 1 8.44
CHEMBL3609353 1 8.32
CHEMBL3609358 1 8.15
CHEMBL3609354 1 8.14
CHEMBL3609356 1 8.12
CHEMBL3609355 1 7.96
CHEMBL3609351 1 7.89
CHEMBL3609352 1 7.33
CHEMBL15988 1 6.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3609360 Ki = 0.61 nM 9.21
CHEMBL3609359 Ki = 2.1 nM 8.68
CHEMBL1188811 Ki = 3.0 nM 8.52
CHEMBL3609357 Ki = 3.6 nM 8.44
CHEMBL3609353 Ki = 4.8 nM 8.32
CHEMBL3609358 Ki = 7.1 nM 8.15
CHEMBL3609354 Ki = 7.2 nM 8.14
CHEMBL3609356 Ki = 7.5 nM 8.12
CHEMBL3609355 Ki = 11.0 nM 7.96
CHEMBL3609351 Ki = 13.0 nM 7.89
CHEMBL3609352 Ki = 47.0 nM 7.33
CHEMBL15988 Ki = 440.0 nM 6.36