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Assay Detail

CHEMBL678745

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

Binding
Binding affinity for human GABA-A receptor alpha-5-beta-3-gamma-2 subunits in L(tk-) cells
ChEMBL ↗
62
Total Activities
62
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

GABA-A receptor; alpha-5/beta-3/gamma-2 (CHEMBL2094122) ↗
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor ligands with alpha 2, alpha 3, and alpha 5-subtype binding selectivity over alpha 1.
Carling RW, Moore KW, Street LJ, Wild D, Isted C, Leeson PD, Thomas S, O'Connor D, McKernan RM, Quirk K, Cook SM, Atack JR, Wafford KA, Thompson SA, Dawson GR, Ferris P, Castro JL.
J Med Chem (2004) 47 : 1807 -1822
PubMed 15027873 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 62 7.99 9.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL300615 — — 1 9.82
CHEMBL299210 — — 1 9.77
CHEMBL52672 — — 1 9.48
CHEMBL299611 — — 1 9.48
CHEMBL300862 — — 1 9.44
CHEMBL53238 — — 1 9.42
CHEMBL52030 — — 1 9.40
CHEMBL292380 — — 1 9.30
CHEMBL296607 — — 1 9.19
CHEMBL301063 — — 1 9.13
CHEMBL300951 — — 1 9.08
CHEMBL298386 — — 1 9.06
CHEMBL296383 — — 1 9.04
CHEMBL300497 — — 1 8.96
CHEMBL53587 — — 1 8.92
CHEMBL292462 — — 1 8.77
CHEMBL416659 — — 1 8.60
CHEMBL301181 — — 1 8.57
CHEMBL299802 — — 1 8.49
CHEMBL50402 — — 1 8.43
CHEMBL441612 — — 1 8.40
CHEMBL298760 — — 1 8.29
CHEMBL53529 — — 1 8.10
CHEMBL12 DIAZEPAM 4.0 1 7.96
CHEMBL52310 — — 1 7.89
CHEMBL50320 — — 1 7.82
CHEMBL299736 — — 1 7.80
CHEMBL301336 — — 1 7.75
CHEMBL441978 — — 1 7.72
CHEMBL299642 — — 1 7.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL300615 — Ki = 0.15 nM 9.82
CHEMBL299210 — Ki = 0.17 nM 9.77
CHEMBL299611 — Ki = 0.33 nM 9.48
CHEMBL52672 — Ki = 0.33 nM 9.48
CHEMBL300862 — Ki = 0.36 nM 9.44
CHEMBL53238 — Ki = 0.38 nM 9.42
CHEMBL52030 — Ki = 0.4 nM 9.40
CHEMBL292380 — Ki = 0.5 nM 9.30
CHEMBL296607 — Ki = 0.64 nM 9.19
CHEMBL301063 — Ki = 0.74 nM 9.13
CHEMBL300951 — Ki = 0.84 nM 9.08
CHEMBL298386 — Ki = 0.88 nM 9.06
CHEMBL296383 — Ki = 0.92 nM 9.04
CHEMBL300497 — Ki = 1.1 nM 8.96
CHEMBL53587 — Ki = 1.2 nM 8.92
CHEMBL292462 — Ki = 1.7 nM 8.77
CHEMBL416659 — Ki = 2.5 nM 8.60
CHEMBL301181 — Ki = 2.7 nM 8.57
CHEMBL299802 — Ki = 3.2 nM 8.49
CHEMBL50402 — Ki = 3.7 nM 8.43
CHEMBL441612 — Ki = 4.0 nM 8.40
CHEMBL298760 — Ki = 5.1 nM 8.29
CHEMBL53529 — Ki = 8.0 nM 8.10
CHEMBL12 DIAZEPAM Ki = 11.0 nM 7.96
CHEMBL52310 — Ki = 13.0 nM 7.89
CHEMBL50320 — Ki = 15.0 nM 7.82
CHEMBL299736 — Ki = 16.0 nM 7.80
CHEMBL301336 — Ki = 18.0 nM 7.75
CHEMBL441978 — Ki = 19.0 nM 7.72
CHEMBL299642 — Ki = 20.0 nM 7.70
CHEMBL53729 — Ki = 29.0 nM 7.54
CHEMBL55450 — Ki = 30.0 nM 7.52
CHEMBL299437 — Ki = 31.0 nM 7.51
CHEMBL50581 — Ki = 38.0 nM 7.42
CHEMBL300018 — Ki = 39.0 nM 7.41
CHEMBL297717 — Ki = 72.0 nM 7.14
CHEMBL298501 — Ki = 74.0 nM 7.13
CHEMBL273456 — Ki = 80.0 nM 7.10
CHEMBL53642 — Ki = 130.0 nM 6.89
CHEMBL52818 — Ki = 140.0 nM 6.85
CHEMBL52640 — Ki = 150.0 nM 6.82
CHEMBL300867 — Ki = 160.0 nM 6.80
CHEMBL51911 — Ki = 160.0 nM 6.80
CHEMBL445358 — Ki = 170.0 nM 6.77
CHEMBL52696 — Ki = 170.0 nM 6.77
CHEMBL297958 — Ki = 240.0 nM 6.62
CHEMBL300690 — Ki = 250.0 nM 6.60
CHEMBL13662 CI-218872 Ki = 560.0 nM 6.25
CHEMBL55081 — Ki = 560.0 nM 6.25
CHEMBL54859 — Ki = 4800.0 nM 5.32