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Assay Detail

CHEMBL643759

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

Binding
Inhibition of [3H]prazosin binding to CHO-K1 whole cells expressing human cloned Alpha-1A adrenergic receptor
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO-K1
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Alpha-1A adrenergic receptor (CHEMBL229)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis, pharmacology and pharmacokinetics of 3-(4-aryl-piperazin-1-ylalkyl)-uracils as uroselective alpha1A-antagonists.
Lopez FJ, Arias L, Chan R, Clarke DE, Elworthy TR, Ford AP, Guzman A, Jaime-Figueroa S, Jasper JR, Morgans DJ, Padilla F, Perez-Medrano A, Quintero C, Romero M, Sandoval L, Smith SA, Williams TJ, Blue DR.
Bioorg Med Chem Lett (2003) 13 : 1873 -1878
PubMed 12749888 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 9.00 10.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL292189 1 10.40
CHEMBL56863 1 10.20
CHEMBL55695 1 9.80
CHEMBL417954 1 9.60
CHEMBL56331 1 9.60
CHEMBL55290 1 9.50
CHEMBL293149 1 9.30
CHEMBL55629 1 9.10
CHEMBL53675 1 9.10
CHEMBL59153 1 9.00
CHEMBL298838 1 9.00
CHEMBL24777 1 8.90
CHEMBL299452 1 8.90
CHEMBL418112 1 8.80
CHEMBL56489 1 8.80
CHEMBL292403 1 8.70
CHEMBL57740 1 8.60
CHEMBL417758 1 8.40
CHEMBL56375 1 8.30
CHEMBL291951 1 8.20
CHEMBL55645 1 8.10
CHEMBL301650 1 7.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL292189 Ki = 0.03981 nM 10.40
CHEMBL56863 Ki = 0.0631 nM 10.20
CHEMBL55695 Ki = 0.1585 nM 9.80
CHEMBL417954 Ki = 0.2512 nM 9.60
CHEMBL56331 Ki = 0.2512 nM 9.60
CHEMBL55290 Ki = 0.3162 nM 9.50
CHEMBL293149 Ki = 0.5012 nM 9.30
CHEMBL55629 Ki = 0.7943 nM 9.10
CHEMBL53675 Ki = 0.7943 nM 9.10
CHEMBL59153 Ki = 1.0 nM 9.00
CHEMBL298838 Ki = 1.0 nM 9.00
CHEMBL24777 Ki = 1.259 nM 8.90
CHEMBL299452 Ki = 1.259 nM 8.90
CHEMBL418112 Ki = 1.585 nM 8.80
CHEMBL56489 Ki = 1.585 nM 8.80
CHEMBL292403 Ki = 1.995 nM 8.70
CHEMBL57740 Ki = 2.512 nM 8.60
CHEMBL417758 Ki = 3.981 nM 8.40
CHEMBL56375 Ki = 5.012 nM 8.30
CHEMBL291951 Ki = 6.31 nM 8.20
CHEMBL55645 Ki = 7.943 nM 8.10
CHEMBL301650 Ki = 19.95 nM 7.70