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Assay Detail

CHEMBL642129

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-1D adrenergic receptor
19
Total Activities
19
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-1D adrenergic receptor (CHEMBL223)
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 19 7.65 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL56863 1 8.70
CHEMBL293149 1 8.60
CHEMBL292189 1 8.30
CHEMBL55290 1 8.10
CHEMBL298838 1 8.00
CHEMBL56331 1 7.90
CHEMBL55629 1 7.80
CHEMBL292403 1 7.70
CHEMBL53675 1 7.60
CHEMBL417954 1 7.60
CHEMBL418112 1 7.50
CHEMBL59153 1 7.50
CHEMBL299452 1 7.50
CHEMBL56489 1 7.30
CHEMBL24777 1 7.20
CHEMBL55645 1 7.20
CHEMBL291951 1 7.00
CHEMBL417758 1 6.90
CHEMBL56375 1 6.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL56863 Ki = 1.995 nM 8.70
CHEMBL293149 Ki = 2.512 nM 8.60
CHEMBL292189 Ki = 5.012 nM 8.30
CHEMBL55290 Ki = 7.943 nM 8.10
CHEMBL298838 Ki = 10.0 nM 8.00
CHEMBL56331 Ki = 12.59 nM 7.90
CHEMBL55629 Ki = 15.85 nM 7.80
CHEMBL292403 Ki = 19.95 nM 7.70
CHEMBL53675 Ki = 25.12 nM 7.60
CHEMBL417954 Ki = 25.12 nM 7.60
CHEMBL418112 Ki = 31.62 nM 7.50
CHEMBL59153 Ki = 31.62 nM 7.50
CHEMBL299452 Ki = 31.62 nM 7.50
CHEMBL56489 Ki = 50.12 nM 7.30
CHEMBL24777 Ki = 63.1 nM 7.20
CHEMBL55645 Ki = 63.1 nM 7.20
CHEMBL291951 Ki = 100.0 nM 7.00
CHEMBL417758 Ki = 125.89 nM 6.90
CHEMBL56375 Ki = 125.89 nM 6.90