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Assay Detail

CHEMBL642984

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

Binding
Affinity to human Alpha-1D adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

2-(Anilinomethyl)imidazolines as alpha1 adrenergic receptor agonists: the discovery of alpha1a subtype selective 2'-alkylsulfonyl-substituted analogues.
Hodson SJ, Bishop MJ, Speake JD, Navas F, Garrison DT, Bigham EC, Saussy DL, Liacos JA, Irving PE, Gobel MJ, Sherman BW.
J Med Chem (2002) 45 : 2229 -2239
PubMed 12014961 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 26 6.40 8.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL70751 1 8.33
CHEMBL306792 1 8.30
CHEMBL72768 1 8.21
CHEMBL540542 1 7.95
CHEMBL72441 1 7.76
CHEMBL540035 1 7.24
CHEMBL70691 1 6.97
CHEMBL553276 1 6.65
CHEMBL70692 1 6.52
CHEMBL72724 1 6.32
CHEMBL70563 1 6.06
CHEMBL74114 1 6.04
CHEMBL542402 1 5.92
CHEMBL762 OXYMETAZOLINE 4.0 1 5.87
CHEMBL554416 1 5.86
CHEMBL70326 1 5.79
CHEMBL70973 1 5.65
CHEMBL70634 1 5.62
CHEMBL74467 1 5.58
CHEMBL74071 1 5.55
CHEMBL419448 1 5.46
CHEMBL544290 1 5.42
CHEMBL71479 1 5.32
CHEMBL71001 1 5.12
CHEMBL302698 1 -
CHEMBL70740 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL70751 Ki = 4.677 nM 8.33
CHEMBL306792 Ki = 5.012 nM 8.30
CHEMBL72768 Ki = 6.166 nM 8.21
CHEMBL540542 Ki = 11.22 nM 7.95
CHEMBL72441 Ki = 17.38 nM 7.76
CHEMBL540035 Ki = 57.54 nM 7.24
CHEMBL70691 Ki = 107.15 nM 6.97
CHEMBL553276 Ki = 223.87 nM 6.65
CHEMBL70692 Ki = 302.0 nM 6.52
CHEMBL72724 Ki = 478.63 nM 6.32
CHEMBL70563 Ki = 870.96 nM 6.06
CHEMBL74114 Ki = 912.01 nM 6.04
CHEMBL542402 Ki = 1202.26 nM 5.92
CHEMBL762 OXYMETAZOLINE Ki = 1348.96 nM 5.87
CHEMBL554416 Ki = 1380.38 nM 5.86
CHEMBL70326 Ki = 1621.81 nM 5.79
CHEMBL70973 Ki = 2238.72 nM 5.65
CHEMBL70634 Ki = 2398.83 nM 5.62
CHEMBL74467 Ki = 2630.27 nM 5.58
CHEMBL74071 Ki = 2818.38 nM 5.55
CHEMBL419448 Ki = 3467.37 nM 5.46
CHEMBL544290 Ki = 3801.89 nM 5.42
CHEMBL71479 Ki = 4786.3 nM 5.32
CHEMBL71001 Ki = 7585.78 nM 5.12
CHEMBL302698 Ki < 15848.93 nM -
CHEMBL70740 Ki < 15848.93 nM -