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Assay Detail

CHEMBL647284

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

Binding
Binding affinity was determined for the alpha-1B adrenergic receptor
30
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design and synthesis of novel alpha1a adrenoceptor-selective dihydropyridine antagonists for the treatment of benign prostatic hyperplasia.
Nagarathnam D, Wetzel JM, Miao SW, Marzabadi MR, Chiu G, Wong WC, Hong X, Fang J, Forray C, Branchek TA, Heydorn WE, Chang RS, Broten T, Schorn TW, Gluchowski C.
J Med Chem (1998) 41 : 5320 -5333
PubMed 9857099 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 30 5.74 9.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2 PRAZOSIN 4.0 1 9.26
CHEMBL358406 1 6.81
CHEMBL358253 1 6.67
CHEMBL279436 1 6.48
CHEMBL346649 1 6.41
CHEMBL359375 1 6.28
CHEMBL151825 1 6.28
CHEMBL41844 1 6.16
CHEMBL148552 1 6.14
CHEMBL347559 1 5.99
CHEMBL347499 1 5.93
CHEMBL146815 1 5.93
CHEMBL357061 1 5.80
CHEMBL347501 1 5.80
CHEMBL151045 1 5.72
CHEMBL151878 1 5.57
CHEMBL356829 1 5.56
CHEMBL357681 1 5.51
CHEMBL149263 1 5.47
CHEMBL147077 3 5.44
CHEMBL355910 1 5.41
CHEMBL347522 1 5.28
CHEMBL356623 1 5.26
CHEMBL150696 1 4.61
CHEMBL151668 1 4.54
CHEMBL150743 1 4.40
CHEMBL146983 1 4.40
CHEMBL356923 1 4.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2 PRAZOSIN Ki = 0.55 nM 9.26
CHEMBL358406 Ki = 156.0 nM 6.81
CHEMBL358253 Ki = 215.0 nM 6.67
CHEMBL279436 Ki = 330.0 nM 6.48
CHEMBL346649 Ki = 390.0 nM 6.41
CHEMBL359375 Ki = 530.0 nM 6.28
CHEMBL151825 Ki = 520.0 nM 6.28
CHEMBL41844 Ki = 700.0 nM 6.16
CHEMBL148552 Ki = 720.0 nM 6.14
CHEMBL347559 Ki = 1020.0 nM 5.99
CHEMBL347499 Ki = 1180.0 nM 5.93
CHEMBL146815 Ki = 1180.0 nM 5.93
CHEMBL357061 Ki = 1570.0 nM 5.80
CHEMBL347501 Ki = 1600.0 nM 5.80
CHEMBL151045 Ki = 1890.0 nM 5.72
CHEMBL151878 Ki = 2720.0 nM 5.57
CHEMBL356829 Ki = 2740.0 nM 5.56
CHEMBL357681 Ki = 3070.0 nM 5.51
CHEMBL149263 Ki = 3410.0 nM 5.47
CHEMBL147077 Ki = 3660.0 nM 5.44
CHEMBL355910 Ki = 3920.0 nM 5.41
CHEMBL147077 Ki = 4920.0 nM 5.31
CHEMBL147077 Ki = 5170.0 nM 5.29
CHEMBL347522 Ki = 5250.0 nM 5.28
CHEMBL356623 Ki = 5500.0 nM 5.26
CHEMBL150696 Ki = 24400.0 nM 4.61
CHEMBL151668 Ki = 29000.0 nM 4.54
CHEMBL150743 Ki = 39500.0 nM 4.40
CHEMBL146983 Ki = 39500.0 nM 4.40
CHEMBL356923 Ki = 45000.0 nM 4.35