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Assay Detail

CHEMBL647046

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

Binding
Inhibition of binding of [125I]HEAT to cloned human alpha-1A adrenergic receptor.
29
Total Activities
27
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 (CHEMBL229)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Phenylacetamides as selective alpha-1A adrenergic receptor antagonists.
Patane MA, DiPardo RM, Newton RC, Price RP, Broten TP, Chang RS, Ransom RW, Di Salvo J, Nagarathnam D, Forray C, Gluchowski C, Bock MG.
Bioorg Med Chem Lett (2000) 10 : 1621 -1624
PubMed 10937709 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 29 7.79 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL44294 1 9.00
CHEMBL415887 1 8.96
CHEMBL298058 1 8.89
CHEMBL41994 3 8.70
CHEMBL42514 1 8.47
CHEMBL41844 1 8.44
CHEMBL41677 1 8.29
CHEMBL289339 1 8.19
CHEMBL44124 1 8.14
CHEMBL297667 1 8.13
CHEMBL42220 1 8.12
CHEMBL295304 1 8.06
CHEMBL435576 1 7.92
CHEMBL42763 1 7.66
CHEMBL417350 1 7.62
CHEMBL432302 1 7.60
CHEMBL289916 1 7.57
CHEMBL296965 1 7.55
CHEMBL44496 1 7.33
CHEMBL416073 1 7.30
CHEMBL40303 1 7.21
CHEMBL42361 1 7.14
CHEMBL43799 1 7.13
CHEMBL43749 1 7.12
CHEMBL42156 1 6.62
CHEMBL41959 1 6.42
CHEMBL44288 1 6.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL44294 Ki = 0.99 nM 9.00
CHEMBL415887 Ki = 1.1 nM 8.96
CHEMBL298058 Ki = 1.3 nM 8.89
CHEMBL41994 Ki = 2.0 nM 8.70
CHEMBL41994 Ki = 2.0 nM 8.70
CHEMBL42514 Ki = 3.4 nM 8.47
CHEMBL41844 Ki = 3.6 nM 8.44
CHEMBL41677 Ki = 5.1 nM 8.29
CHEMBL289339 Ki = 6.4 nM 8.19
CHEMBL44124 Ki = 7.3 nM 8.14
CHEMBL297667 Ki = 7.4 nM 8.13
CHEMBL42220 Ki = 7.5 nM 8.12
CHEMBL295304 Ki = 8.8 nM 8.06
CHEMBL435576 Ki = 12.0 nM 7.92
CHEMBL42763 Ki = 22.0 nM 7.66
CHEMBL417350 Ki = 24.0 nM 7.62
CHEMBL432302 Ki = 25.0 nM 7.60
CHEMBL289916 Ki = 27.0 nM 7.57
CHEMBL296965 Ki = 28.0 nM 7.55
CHEMBL44496 Ki = 47.0 nM 7.33
CHEMBL41994 Ki = 50.0 nM 7.30
CHEMBL416073 Ki = 50.0 nM 7.30
CHEMBL40303 Ki = 61.0 nM 7.21
CHEMBL42361 Ki = 72.0 nM 7.14
CHEMBL43799 Ki = 74.0 nM 7.13
CHEMBL43749 Ki = 75.0 nM 7.12
CHEMBL42156 Ki = 240.0 nM 6.62
CHEMBL41959 Ki = 380.0 nM 6.42
CHEMBL44288 Ki = 570.0 nM 6.24