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Assay Detail

CHEMBL646108

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

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

Assay Information

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

Target

Alpha-1D adrenergic receptor (CHEMBL223)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Arylpiperazine substituted heterocycles as selective alpha(1a) adrenergic antagonists.
Khatuya H, Hutchings RH, Kuo GH, Pulito VL, Jolliffe LK, Li X, Murray WV.
Bioorg Med Chem Lett (2002) 12 : 2443 -2446
PubMed 12161153 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 6.50 7.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL80109 1 7.46
CHEMBL310890 1 7.40
CHEMBL309969 1 7.18
CHEMBL310768 1 6.98
CHEMBL81661 1 6.77
CHEMBL79817 1 6.54
CHEMBL79990 1 5.96
CHEMBL81093 1 5.84
CHEMBL80125 1 5.51
CHEMBL80036 1 5.38
CHEMBL79940 1 -
CHEMBL83791 1 -
CHEMBL82480 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL80109 Ki = 34.5 nM 7.46
CHEMBL310890 Ki = 39.5 nM 7.40
CHEMBL309969 Ki = 65.5 nM 7.18
CHEMBL310768 Ki = 105.0 nM 6.98
CHEMBL81661 Ki = 170.0 nM 6.77
CHEMBL79817 Ki = 285.0 nM 6.54
CHEMBL79990 Ki = 1107.0 nM 5.96
CHEMBL81093 Ki = 1435.0 nM 5.84
CHEMBL80125 Ki = 3064.0 nM 5.51
CHEMBL80036 Ki = 4142.0 nM 5.38
CHEMBL79940 Ki > 5000.0 nM -
CHEMBL83791 Ki > 5000.0 nM -
CHEMBL82480 Ki > 5000.0 nM -