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Assay Detail

CHEMBL640501

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

Binding
Affinity to human Alpha-2A adrenergic receptor determined by radioligand binding techniques from chinese hamster ovary (CHO) cells
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Alpha-2A adrenergic receptor (CHEMBL1867)
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 25 6.44 7.79

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL762 OXYMETAZOLINE 4.0 1 7.79
CHEMBL72768 1 7.74
CHEMBL70751 1 7.38
CHEMBL540542 1 7.32
CHEMBL306792 1 7.23
CHEMBL72441 1 7.20
CHEMBL540035 1 7.09
CHEMBL553276 1 7.09
CHEMBL70692 1 6.78
CHEMBL72724 1 6.70
CHEMBL70691 1 6.66
CHEMBL70326 1 6.40
CHEMBL70740 1 6.10
CHEMBL74114 1 6.06
CHEMBL542402 1 6.01
CHEMBL70973 1 5.88
CHEMBL74071 1 5.53
CHEMBL71001 1 5.44
CHEMBL71479 1 5.41
CHEMBL74467 1 5.35
CHEMBL70563 1 5.30
CHEMBL544290 1 5.25
CHEMBL419448 1 -
CHEMBL70634 1 -
CHEMBL302698 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL762 OXYMETAZOLINE Ki = 16.22 nM 7.79
CHEMBL72768 Ki = 18.2 nM 7.74
CHEMBL70751 Ki = 41.69 nM 7.38
CHEMBL540542 Ki = 47.86 nM 7.32
CHEMBL306792 Ki = 58.88 nM 7.23
CHEMBL72441 Ki = 63.1 nM 7.20
CHEMBL540035 Ki = 81.28 nM 7.09
CHEMBL553276 Ki = 81.28 nM 7.09
CHEMBL70692 Ki = 165.96 nM 6.78
CHEMBL72724 Ki = 199.53 nM 6.70
CHEMBL70691 Ki = 218.78 nM 6.66
CHEMBL70326 Ki = 398.11 nM 6.40
CHEMBL70740 Ki = 794.33 nM 6.10
CHEMBL74114 Ki = 870.96 nM 6.06
CHEMBL542402 Ki = 977.24 nM 6.01
CHEMBL70973 Ki = 1318.26 nM 5.88
CHEMBL74071 Ki = 2951.21 nM 5.53
CHEMBL71001 Ki = 3630.78 nM 5.44
CHEMBL71479 Ki = 3890.45 nM 5.41
CHEMBL74467 Ki = 4466.84 nM 5.35
CHEMBL70563 Ki = 5011.87 nM 5.30
CHEMBL544290 Ki = 5623.41 nM 5.25
CHEMBL419448 Ki < 7943.28 nM -
CHEMBL70634 Ki < 7943.28 nM -
CHEMBL302698 Ki < 7943.28 nM -