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Assay Detail

CHEMBL649156

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

Binding
Inhibition of [3H]prazosin binding to human Alpha-1B adrenergic receptor expressed in CHO cells
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications.
Ruffolo RR, Bondinell W, Hieble JP.
J Med Chem (1995) 38 : 3681 -3716
PubMed 7562902 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 6.64 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL123448 1 7.82
CHEMBL25467 1 7.64
CHEMBL3392246 1 7.07
CHEMBL405355 NIGULDIPINE 2.0 1 7.07
CHEMBL114166 1 7.06
CHEMBL3392247 1 6.63
CHEMBL5483012 1 6.57
CHEMBL279436 1 6.39
CHEMBL284103 1 6.38
CHEMBL123349 1 6.31
CHEMBL31410 CORYNANTHEINE 1 6.29
CHEMBL123138 1 6.11
CHEMBL15245 YOHIMBINE 3.0 1 6.01
CHEMBL10347 RAUWOLSCINE 1 5.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL123448 Ki = 15.0 nM 7.82
CHEMBL25467 Ki = 23.0 nM 7.64
CHEMBL3392246 Ki = 85.0 nM 7.07
CHEMBL405355 NIGULDIPINE Ki = 85.0 nM 7.07
CHEMBL114166 Ki = 87.0 nM 7.06
CHEMBL3392247 Ki = 234.0 nM 6.63
CHEMBL5483012 Ki = 269.0 nM 6.57
CHEMBL279436 Ki = 407.0 nM 6.39
CHEMBL284103 Ki = 416.0 nM 6.38
CHEMBL123349 Ki = 485.0 nM 6.31
CHEMBL31410 CORYNANTHEINE Ki = 517.0 nM 6.29
CHEMBL123138 Ki = 783.0 nM 6.11
CHEMBL15245 YOHIMBINE Ki = 966.0 nM 6.01
CHEMBL10347 RAUWOLSCINE Ki = 2270.0 nM 5.64