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Assay Detail

CHEMBL913649

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

Binding
Displacement of [125I]BE2254 from human cloned adrenergic alpha 1D receptor expressed in HEK293 cells
12
Total Activities
12
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

New pyrimido[5,4-b]indoles and [1]benzothieno[3,2-d]pyrimidines: high affinity ligands for the alpha(1)-adrenoceptor subtypes.
Romeo G, Materia L, Marucci G, Modica M, Pittalà V, Salerno L, Siracusa MA, Buccioni M, Angeli P, Minneman KP.
Bioorg Med Chem Lett (2006) 16 : 6200 -6203
PubMed 17027264 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 8.52 9.78
Log Ki 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL220515 1 9.78
CHEMBL301707 1 9.44
CHEMBL220221 1 9.40
CHEMBL99142 1 9.39
CHEMBL222896 1 9.08
CHEMBL220781 1 8.90
CHEMBL386005 1 8.81
CHEMBL220717 1 8.13
CHEMBL223289 1 7.87
CHEMBL219718 1 6.51
CHEMBL219719 1 6.36
CHEMBL223842 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL220515 Ki = 0.166 nM 9.78
CHEMBL301707 Ki = 0.3631 nM 9.44
CHEMBL220221 Ki = 0.3981 nM 9.40
CHEMBL99142 Ki = 0.4074 nM 9.39
CHEMBL222896 Ki = 0.8318 nM 9.08
CHEMBL220781 Ki = 1.259 nM 8.90
CHEMBL386005 Ki = 1.549 nM 8.81
CHEMBL220717 Ki = 7.413 nM 8.13
CHEMBL223289 Ki = 13.49 nM 7.87
CHEMBL219718 Ki = 309.03 nM 6.51
CHEMBL219719 Ki = 436.52 nM 6.36
CHEMBL223842 Log Ki - -