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Assay Detail

CHEMBL644674

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

Functional
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Design, synthesis, and biological activity of prazosin-related antagonists. Role of the piperazine and furan units of prazosin on the selectivity for alpha1-adrenoreceptor subtypes.
Bolognesi ML, Budriesi R, Chiarini A, Poggesi E, Leonardi A, Melchiorre C.
J Med Chem (1998) 41 : 4844 -4853
PubMed 9822553 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 21 7.46 9.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL27013 1 9.04
CHEMBL2 PRAZOSIN 4.0 1 8.60
CHEMBL144238 1 8.17
CHEMBL144000 1 8.05
CHEMBL144776 1 7.97
CHEMBL148061 1 7.82
CHEMBL145181 1 7.78
CHEMBL29591 1 7.53
CHEMBL144224 1 7.42
CHEMBL342997 1 7.41
CHEMBL357669 1 7.32
CHEMBL341665 1 7.26
CHEMBL144768 1 7.23
CHEMBL144263 1 7.14
CHEMBL358060 1 7.11
CHEMBL145384 1 7.10
CHEMBL146724 1 7.04
CHEMBL13647 BMY-7378 1 6.94
CHEMBL138681 1 6.72
CHEMBL146601 1 6.70
CHEMBL144677 1 6.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL27013 Kd = 0.912 nM 9.04
CHEMBL2 PRAZOSIN Kd = 2.512 nM 8.60
CHEMBL144238 Kd = 6.761 nM 8.17
CHEMBL144000 Kd = 8.913 nM 8.05
CHEMBL144776 Kd = 10.72 nM 7.97
CHEMBL148061 Kd = 15.14 nM 7.82
CHEMBL145181 Kd = 16.6 nM 7.78
CHEMBL29591 Kd = 29.51 nM 7.53
CHEMBL144224 Kd = 38.02 nM 7.42
CHEMBL342997 Kd = 38.9 nM 7.41
CHEMBL357669 Kd = 47.86 nM 7.32
CHEMBL341665 Kd = 54.95 nM 7.26
CHEMBL144768 Kd = 58.88 nM 7.23
CHEMBL144263 Kd = 72.44 nM 7.14
CHEMBL358060 Kd = 77.62 nM 7.11
CHEMBL145384 Kd = 79.43 nM 7.10
CHEMBL146724 Kd = 91.2 nM 7.04
CHEMBL13647 BMY-7378 Kd = 114.82 nM 6.94
CHEMBL138681 Kd = 190.55 nM 6.72
CHEMBL146601 Kd = 199.53 nM 6.70
CHEMBL144677 Kd = 416.87 nM 6.38