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Assay Detail

CHEMBL1798145

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

Binding
Displacement of [125I]BE-2254 from human adrenergic Alpha-1D receptor expressed in HEK293 cells
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Novel 4-phenylpiperidine-2,6-dione derivatives. Ligands for α₁-adrenoceptor subtypes.
Romeo G, Materia L, Modica MN, Pittalà V, Salerno L, Siracusa MA, Manetti F, Botta M, Minneman KP.
Eur J Med Chem (2011) 46 : 2676 -2690
PubMed 21514979 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 29 7.23 9.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL56438 1 9.89
CHEMBL301707 1 9.44
CHEMBL1796046 1 7.84
CHEMBL1796033 1 7.80
CHEMBL1796050 1 7.79
CHEMBL319972 1 7.70
CHEMBL1796036 1 7.51
CHEMBL1796034 1 7.47
CHEMBL100434 1 7.45
CHEMBL1796035 1 7.41
CHEMBL1796031 1 7.36
CHEMBL1796030 1 7.34
CHEMBL1796044 1 7.29
CHEMBL1796043 1 7.27
CHEMBL95191 1 7.22
CHEMBL1796040 1 7.20
CHEMBL1796042 1 7.17
CHEMBL1796039 1 7.16
CHEMBL1796041 1 7.14
CHEMBL1796049 1 7.12
CHEMBL1796047 1 7.11
CHEMBL1796045 1 7.01
CHEMBL330198 1 6.61
CHEMBL1796032 1 6.41
CHEMBL1796029 1 6.20
CHEMBL1796037 1 6.16
CHEMBL1796048 1 6.04
CHEMBL1796028 1 5.88
CHEMBL1796038 1 5.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL56438 Ki = 0.1288 nM 9.89
CHEMBL301707 Ki = 0.3631 nM 9.44
CHEMBL1796046 Ki = 14.45 nM 7.84
CHEMBL1796033 Ki = 15.85 nM 7.80
CHEMBL1796050 Ki = 16.22 nM 7.79
CHEMBL319972 Ki = 19.95 nM 7.70
CHEMBL1796036 Ki = 30.9 nM 7.51
CHEMBL1796034 Ki = 33.88 nM 7.47
CHEMBL100434 Ki = 35.48 nM 7.45
CHEMBL1796035 Ki = 38.9 nM 7.41
CHEMBL1796031 Ki = 43.65 nM 7.36
CHEMBL1796030 Ki = 45.71 nM 7.34
CHEMBL1796044 Ki = 51.29 nM 7.29
CHEMBL1796043 Ki = 53.7 nM 7.27
CHEMBL95191 Ki = 60.26 nM 7.22
CHEMBL1796040 Ki = 63.1 nM 7.20
CHEMBL1796042 Ki = 67.61 nM 7.17
CHEMBL1796039 Ki = 69.18 nM 7.16
CHEMBL1796041 Ki = 72.44 nM 7.14
CHEMBL1796049 Ki = 75.86 nM 7.12
CHEMBL1796047 Ki = 77.62 nM 7.11
CHEMBL1796045 Ki = 97.72 nM 7.01
CHEMBL330198 Ki = 245.47 nM 6.61
CHEMBL1796032 Ki = 389.05 nM 6.41
CHEMBL1796029 Ki = 630.96 nM 6.20
CHEMBL1796037 Ki = 691.83 nM 6.16
CHEMBL1796048 Ki = 912.01 nM 6.04
CHEMBL1796028 Ki = 1318.26 nM 5.88
CHEMBL1796038 Ki = 1513.56 nM 5.82