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Assay Detail

CHEMBL652815

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

Binding
Displacement of [125I]HEAT from COS cell membranes expressing human Alpha-1A adrenergic receptor
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type COS
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Novel thiophene derivatives for the treatment of benign prostatic hyperplasia.
Khatuya H, Pulito VL, Jolliffe LK, Li X, Murray WV.
Bioorg Med Chem Lett (2002) 12 : 2145 -2148
PubMed 12127524 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 7.76 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL69848 1 9.70
CHEMBL305029 1 9.52
CHEMBL67713 1 9.30
CHEMBL421297 1 8.74
CHEMBL68241 1 7.92
CHEMBL420184 1 7.85
CHEMBL69339 1 7.75
CHEMBL70178 1 7.40
CHEMBL67932 1 6.89
CHEMBL302495 1 6.70
CHEMBL303485 1 6.48
CHEMBL66823 1 6.38
CHEMBL418882 1 6.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL69848 Ki = 0.2 nM 9.70
CHEMBL305029 Ki = 0.3 nM 9.52
CHEMBL67713 Ki = 0.5 nM 9.30
CHEMBL421297 Ki = 1.8 nM 8.74
CHEMBL68241 Ki = 12.0 nM 7.92
CHEMBL420184 Ki = 14.0 nM 7.85
CHEMBL69339 Ki = 18.0 nM 7.75
CHEMBL70178 Ki = 40.0 nM 7.40
CHEMBL67932 Ki = 128.0 nM 6.89
CHEMBL302495 Ki = 202.0 nM 6.70
CHEMBL303485 Ki = 331.0 nM 6.48
CHEMBL66823 Ki = 419.0 nM 6.38
CHEMBL418882 Ki = 578.0 nM 6.24