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Assay Detail

CHEMBL647272

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

Binding
Effective concentration in vitro against rat spleen Alpha-1B adrenergic receptor indicates EC50 < 15% at a concentration of 10 uM
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Spleen
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Alpha-1B adrenergic receptor (CHEMBL315)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine.
Altenbach RJ, Khilevich A, Meyer MD, Buckner SA, Milicic I, Daza AV, Brune ME, O'Neill AB, Gauvin DM, Cain JC, Nakane M, Holladay MW, Williams M, Brioni JD, Sullivan JP.
J Med Chem (2002) 45 : 4395 -4397
PubMed 12238918 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 5.29 6.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL109783 1 6.50
CHEMBL1076 DESGLYMIDODRINE -1.0 1 4.07
CHEMBL136560 (1R,2S)-PHENYLPROPANOLAMINE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL109783 EC50 = 320.0 nM 6.50
CHEMBL1076 DESGLYMIDODRINE EC50 = 85000.0 nM 4.07
CHEMBL136560 (1R,2S)-PHENYLPROPANOLAMINE EC50 = 280000.0 nM -