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Assay Detail

CHEMBL5504542

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

Binding
Binding affinity to human alpha1B-adrenoceptor
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Designing Chromane Derivatives as α<sub>2A</sub>-Adrenoceptor Selective Agonists via Conformation Constraint.
Lv X, Zhou P, Qiao X, Li Y, Yang X, Wang J, He X, Su R.
J Med Chem (2024) 67 : 11435 -11449
PubMed 38889119 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 6.04 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5517941 1 7.70
CHEMBL4594267 TASIPIMIDINE 2.0 1 6.28
CHEMBL134 CLONIDINE 4.0 1 5.13
CHEMBL778 DEXMEDETOMIDINE 4.0 1 5.04
CHEMBL1437 NOREPINEPHRINE 4.0 1 -
CHEMBL862 GUANFACINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5517941 Ki = 19.95 nM 7.70
CHEMBL4594267 TASIPIMIDINE Ki = 524.81 nM 6.28
CHEMBL134 CLONIDINE Ki = 7413.1 nM 5.13
CHEMBL778 DEXMEDETOMIDINE Ki = 9120.11 nM 5.04
CHEMBL1437 NOREPINEPHRINE Ki = 162181.01 nM -
CHEMBL862 GUANFACINE Ki = 134896.29 nM -