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Assay Detail

CHEMBL857772

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

Binding
In vitro binding affinity towards alpha-2B adrenergic receptor of rat neonatal lung in radioligand binding assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Alpha-2B adrenergic receptor (CHEMBL266)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
Altenbach RJ, Khilevich A, Kolasa T, Rohde JJ, Bhatia PA, Patel MV, Searle XB, Yang F, Bunnelle WH, Tietje K, Bayburt EK, Carroll WA, Meyer MD, Henry R, Buckner SA, Kuk J, Daza AV, Milicic IV, Cain JC, Kang CH, Ireland LM, Carr TL, Miller TR, Hancock AA, Nakane M, Esbenshade TA, Brune ME, O'Neill AB, Gauvin DM, Katwala SP, Holladay MW, Brioni JD, Sullivan JP.
J Med Chem (2004) 47 : 3220 -3235
PubMed 15163201 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 6.57 8.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL317912 1 8.42
CHEMBL327116 1 7.65
CHEMBL108804 1 7.32
CHEMBL323402 1 7.31
CHEMBL111771 1 6.73
CHEMBL109783 1 6.61
CHEMBL61006 PHENYLPROPANOLAMINE 4.0 1 6.58
CHEMBL110751 1 6.18
CHEMBL111554 1 6.17
CHEMBL111463 1 6.04
CHEMBL326702 1 6.01
CHEMBL111496 1 5.77
CHEMBL1076 DESGLYMIDODRINE -1.0 1 5.73
CHEMBL109848 1 5.52
CHEMBL321644 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL317912 Ki = 3.802 nM 8.42
CHEMBL327116 Ki = 22.39 nM 7.65
CHEMBL108804 Ki = 47.86 nM 7.32
CHEMBL323402 Ki = 48.98 nM 7.31
CHEMBL111771 Ki = 186.21 nM 6.73
CHEMBL109783 Ki = 245.47 nM 6.61
CHEMBL61006 PHENYLPROPANOLAMINE Ki = 263.03 nM 6.58
CHEMBL110751 Ki = 660.69 nM 6.18
CHEMBL111554 Ki = 676.08 nM 6.17
CHEMBL111463 Ki = 912.01 nM 6.04
CHEMBL326702 Ki = 977.24 nM 6.01
CHEMBL111496 Ki = 1698.24 nM 5.77
CHEMBL1076 DESGLYMIDODRINE Ki = 1862.09 nM 5.73
CHEMBL109848 Ki = 3019.95 nM 5.52
CHEMBL321644 Ki < 10000.0 nM -