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Assay Detail

CHEMBL643448

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

Binding
In vitro inhibitory activity against alpha-1 adrenergic receptor binding to rat brain membranes
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Subcellular Membrane
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Adrenergic receptor alpha-1 (CHEMBL1907610)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

NR2B-selective N-methyl-D-aspartate antagonists: synthesis and evaluation of 5-substituted benzimidazoles.
McCauley JA, Theberge CR, Romano JJ, Billings SB, Anderson KD, Claremon DA, Freidinger RM, Bednar RA, Mosser SD, Gaul SL, Connolly TM, Condra CL, Xia M, Cunningham ME, Bednar B, Stump GL, Lynch JJ, Macaulay A, Wafford KA, Koblan KS, Liverton NJ.
J Med Chem (2004) 47 : 2089 -2096
PubMed 15056006 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 5.73 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL63200 1 6.70
CHEMBL67196 1 6.28
CHEMBL303832 1 6.28
CHEMBL65039 1 6.24
CHEMBL64941 1 6.21
CHEMBL65231 1 6.17
CHEMBL68134 1 6.14
CHEMBL416690 1 6.08
CHEMBL63146 1 5.92
CHEMBL436521 1 5.82
CHEMBL61895 1 5.70
CHEMBL65454 1 5.58
CHEMBL65119 1 5.58
CHEMBL304070 1 5.55
CHEMBL65314 1 5.55
CHEMBL304274 1 5.51
CHEMBL63474 1 5.47
CHEMBL65693 1 5.40
CHEMBL67249 1 5.38
CHEMBL63992 1 5.32
CHEMBL63924 1 5.26
CHEMBL66539 1 4.85
CHEMBL65245 1 4.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL63200 IC50 = 200.0 nM 6.70
CHEMBL67196 IC50 = 530.0 nM 6.28
CHEMBL303832 IC50 = 520.0 nM 6.28
CHEMBL65039 IC50 = 570.0 nM 6.24
CHEMBL64941 IC50 = 620.0 nM 6.21
CHEMBL65231 IC50 = 670.0 nM 6.17
CHEMBL68134 IC50 = 730.0 nM 6.14
CHEMBL416690 IC50 = 830.0 nM 6.08
CHEMBL63146 IC50 = 1200.0 nM 5.92
CHEMBL436521 IC50 = 1500.0 nM 5.82
CHEMBL61895 IC50 = 2000.0 nM 5.70
CHEMBL65454 IC50 = 2600.0 nM 5.58
CHEMBL65119 IC50 = 2600.0 nM 5.58
CHEMBL304070 IC50 = 2800.0 nM 5.55
CHEMBL65314 IC50 = 2800.0 nM 5.55
CHEMBL304274 IC50 = 3100.0 nM 5.51
CHEMBL63474 IC50 = 3400.0 nM 5.47
CHEMBL65693 IC50 = 4000.0 nM 5.40
CHEMBL67249 IC50 = 4200.0 nM 5.38
CHEMBL63992 IC50 = 4800.0 nM 5.32
CHEMBL63924 IC50 = 5500.0 nM 5.26
CHEMBL66539 IC50 = 14000.0 nM 4.85
CHEMBL65245 IC50 = 20000.0 nM 4.70