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Assay Detail

CHEMBL643535

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

Functional
Activity against Alpha-1 adrenergic receptor subtypes of human prostate tissue
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Adrenergic receptor alpha-1 (CHEMBL2094251)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

N-arylpiperazinyl-N'-propylamino derivatives of heteroaryl amides as functional uroselective alpha 1-adrenoceptor antagonists.
Elworthy TR, Ford AP, Bantle GW, Morgans DJ, Ozer RS, Palmer WS, Repke DB, Romero M, Sandoval L, Sjogren EB, Talamás FX, Vazquez A, Wu H, Arredondo NF, Blue DR, DeSousa A, Gross LM, Kava MS, Lesnick JD, Vimont RL, Williams TJ, Zhu QM, Pfister JR, Clarke DE.
J Med Chem (1997) 40 : 2674 -2687
PubMed 9276013 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 6 8.48 10.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL836 TAMSULOSIN 4.0 1 10.40
CHEMBL90874 1 8.70
CHEMBL2 PRAZOSIN 4.0 1 8.70
CHEMBL420060 1 8.20
CHEMBL611 TERAZOSIN 4.0 1 7.60
CHEMBL88272 1 7.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL836 TAMSULOSIN Kd = 0.03981 nM 10.40
CHEMBL90874 Kd = 1.995 nM 8.70
CHEMBL2 PRAZOSIN Kd = 1.995 nM 8.70
CHEMBL420060 Kd = 6.31 nM 8.20
CHEMBL611 TERAZOSIN Kd = 25.12 nM 7.60
CHEMBL88272 Kd = 50.12 nM 7.30