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Assay Detail

CHEMBL652804

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

Binding
In vitro for the displacement of [3H]prazosin binding to bovine Alpha-1A adrenergic receptor
ChEMBL ↗
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Alpha-1A adrenergic receptor (CHEMBL4892) ↗
Type SINGLE PROTEIN
Organism Bos taurus

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
Ki 22 9.11 10.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL91278 — — 1 10.10
CHEMBL88512 — — 1 9.90
CHEMBL836 TAMSULOSIN 4.0 1 9.90
CHEMBL2 PRAZOSIN 4.0 1 9.90
CHEMBL92261 — — 1 9.40
CHEMBL330060 — — 1 9.40
CHEMBL420060 — — 1 9.30
CHEMBL93736 — — 1 9.10
CHEMBL597 PHENTOLAMINE 4.0 1 9.10
CHEMBL91093 — — 1 9.10
CHEMBL88435 — — 1 9.10
CHEMBL88272 — — 1 9.10
CHEMBL91876 — — 1 9.10
CHEMBL90874 — — 1 8.80
CHEMBL92901 — — 1 8.80
CHEMBL89916 — — 1 8.80
CHEMBL88820 — — 1 8.80
CHEMBL90869 — — 1 8.80
CHEMBL90287 — — 1 8.70
CHEMBL611 TERAZOSIN 4.0 1 8.60
CHEMBL312935 — — 1 8.50
CHEMBL92109 — — 1 8.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL91278 — Ki = 0.07943 nM 10.10
CHEMBL88512 — Ki = 0.1259 nM 9.90
CHEMBL836 TAMSULOSIN Ki = 0.1259 nM 9.90
CHEMBL2 PRAZOSIN Ki = 0.1259 nM 9.90
CHEMBL92261 — Ki = 0.3981 nM 9.40
CHEMBL330060 — Ki = 0.3981 nM 9.40
CHEMBL420060 — Ki = 0.5012 nM 9.30
CHEMBL93736 — Ki = 0.7943 nM 9.10
CHEMBL597 PHENTOLAMINE Ki = 0.7943 nM 9.10
CHEMBL91093 — Ki = 0.7943 nM 9.10
CHEMBL88435 — Ki = 0.7943 nM 9.10
CHEMBL88272 — Ki = 0.7943 nM 9.10
CHEMBL91876 — Ki = 0.7943 nM 9.10
CHEMBL90874 — Ki = 1.585 nM 8.80
CHEMBL92901 — Ki = 1.585 nM 8.80
CHEMBL89916 — Ki = 1.585 nM 8.80
CHEMBL88820 — Ki = 1.585 nM 8.80
CHEMBL90869 — Ki = 1.585 nM 8.80
CHEMBL90287 — Ki = 1.995 nM 8.70
CHEMBL611 TERAZOSIN Ki = 2.512 nM 8.60
CHEMBL312935 — Ki = 3.162 nM 8.50
CHEMBL92109 — Ki = 7.943 nM 8.10