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Assay Detail

CHEMBL650874

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

Binding
Binding affinity measured by [3H]diazepam binding assay in rat
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

GABA-A receptor; anion channel (CHEMBL1907607)
Type PROTEIN COMPLEX GROUP
Organism Rattus norvegicus

Publication

2-benzazepines. 5. Synthesis of pyrimido[5,4-d][2]benzazepines and their evaluation as anxiolytic agents.
Trybulski EJ, Benjamin LE, Earley JV, Fryer RI, Gilman NW, Reeder E, Walser A, Davidson AB, Horst WD, Sepinwall J.
J Med Chem (1983) 26 : 1589 -1596
PubMed 6138436 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 32 7.85 8.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL40447 1 8.64
CHEMBL289742 1 8.59
CHEMBL41816 1 8.55
CHEMBL296578 1 8.55
CHEMBL40906 1 8.55
CHEMBL40721 1 8.51
CHEMBL39418 1 8.47
CHEMBL41553 1 8.46
CHEMBL289774 1 8.28
CHEMBL12 DIAZEPAM 4.0 1 8.27
CHEMBL40446 1 8.15
CHEMBL290057 1 8.12
CHEMBL44515 1 8.09
CHEMBL43683 1 8.04
CHEMBL41856 1 8.02
CHEMBL42927 1 8.02
CHEMBL288397 1 7.82
CHEMBL43572 1 7.77
CHEMBL40905 1 7.77
CHEMBL40507 1 7.73
CHEMBL442346 1 7.70
CHEMBL42951 1 7.60
CHEMBL289201 1 7.60
CHEMBL290905 1 7.52
CHEMBL290636 1 7.51
CHEMBL39034 1 7.42
CHEMBL40660 1 7.27
CHEMBL38917 1 7.27
CHEMBL289174 1 7.22
CHEMBL289819 1 6.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL40447 IC50 = 2.3 nM 8.64
CHEMBL289742 IC50 = 2.6 nM 8.59
CHEMBL41816 IC50 = 2.8 nM 8.55
CHEMBL296578 IC50 = 2.8 nM 8.55
CHEMBL40906 IC50 = 2.8 nM 8.55
CHEMBL40721 IC50 = 3.1 nM 8.51
CHEMBL39418 IC50 = 3.4 nM 8.47
CHEMBL41553 IC50 = 3.5 nM 8.46
CHEMBL289774 IC50 = 5.3 nM 8.28
CHEMBL12 DIAZEPAM IC50 = 5.4 nM 8.27
CHEMBL40446 IC50 = 7.1 nM 8.15
CHEMBL290057 IC50 = 7.6 nM 8.12
CHEMBL44515 IC50 = 8.2 nM 8.09
CHEMBL43683 IC50 = 9.2 nM 8.04
CHEMBL42927 IC50 = 9.6 nM 8.02
CHEMBL41856 IC50 = 9.6 nM 8.02
CHEMBL288397 IC50 = 15.0 nM 7.82
CHEMBL43572 IC50 = 17.0 nM 7.77
CHEMBL40905 IC50 = 17.0 nM 7.77
CHEMBL40507 IC50 = 18.5 nM 7.73
CHEMBL442346 IC50 = 20.0 nM 7.70
CHEMBL42951 IC50 = 25.0 nM 7.60
CHEMBL289201 IC50 = 25.0 nM 7.60
CHEMBL290905 IC50 = 30.0 nM 7.52
CHEMBL290636 IC50 = 31.0 nM 7.51
CHEMBL39034 IC50 = 38.0 nM 7.42
CHEMBL40660 IC50 = 54.0 nM 7.27
CHEMBL38917 IC50 = 54.0 nM 7.27
CHEMBL289174 IC50 = 60.0 nM 7.22
CHEMBL289819 IC50 = 140.0 nM 6.85
CHEMBL42809 IC50 = 270.0 nM 6.57
CHEMBL290064 IC50 = 490.0 nM 6.31