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Assay Detail

CHEMBL647201

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

Binding
Affinity to human Alpha-1B adrenergic receptor determined by radioligand binding techniques from rat-1 fibroblasts membranes
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Alpha-1B adrenergic receptor (CHEMBL232)
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 27 6.25 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL306792 1 7.82
CHEMBL72768 1 7.39
CHEMBL540542 1 7.18
CHEMBL70751 1 7.16
CHEMBL540035 1 7.12
CHEMBL72441 1 6.91
CHEMBL553276 1 6.77
CHEMBL70692 1 6.62
CHEMBL74114 1 6.42
CHEMBL70326 1 6.29
CHEMBL70563 1 6.19
CHEMBL70691 1 6.16
CHEMBL542402 1 6.10
CHEMBL554416 1 6.08
CHEMBL762 OXYMETAZOLINE 4.0 1 6.08
CHEMBL70973 1 6.04
CHEMBL74071 1 6.00
CHEMBL544290 1 5.89
CHEMBL74467 1 5.88
CHEMBL72724 1 5.69
CHEMBL70740 1 5.67
CHEMBL419448 1 5.64
CHEMBL70634 1 5.53
CHEMBL71479 1 5.46
CHEMBL71001 1 5.34
CHEMBL72958 NS-49 1 4.95
CHEMBL302698 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL306792 Ki = 15.14 nM 7.82
CHEMBL72768 Ki = 40.74 nM 7.39
CHEMBL540542 Ki = 66.07 nM 7.18
CHEMBL70751 Ki = 69.18 nM 7.16
CHEMBL540035 Ki = 75.86 nM 7.12
CHEMBL72441 Ki = 123.03 nM 6.91
CHEMBL553276 Ki = 169.82 nM 6.77
CHEMBL70692 Ki = 239.88 nM 6.62
CHEMBL74114 Ki = 380.19 nM 6.42
CHEMBL70326 Ki = 512.86 nM 6.29
CHEMBL70563 Ki = 645.65 nM 6.19
CHEMBL70691 Ki = 691.83 nM 6.16
CHEMBL542402 Ki = 794.33 nM 6.10
CHEMBL554416 Ki = 831.76 nM 6.08
CHEMBL762 OXYMETAZOLINE Ki = 831.76 nM 6.08
CHEMBL70973 Ki = 912.01 nM 6.04
CHEMBL74071 Ki = 1000.0 nM 6.00
CHEMBL544290 Ki = 1288.25 nM 5.89
CHEMBL74467 Ki = 1318.26 nM 5.88
CHEMBL72724 Ki = 2041.74 nM 5.69
CHEMBL70740 Ki = 2137.96 nM 5.67
CHEMBL419448 Ki = 2290.87 nM 5.64
CHEMBL70634 Ki = 2951.21 nM 5.53
CHEMBL71479 Ki = 3467.37 nM 5.46
CHEMBL71001 Ki = 4570.88 nM 5.34
CHEMBL72958 NS-49 Ki = 11220.18 nM 4.95
CHEMBL302698 Ki < 10000.0 nM -