Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL681480

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

Binding
Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-5-beta-3-gamma-2
ChEMBL ↗
149
Total Activities
149
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach.
Huang Q, He X, Ma C, Liu R, Yu S, Dayer CA, Wenger GR, McKernan R, Cook JM.
J Med Chem (2000) 43 : 71 -95
PubMed 10633039 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 149 7.84 10.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3144696 — — 1 10.10
CHEMBL3144697 — — 1 9.92
CHEMBL130609 — — 1 9.85
CHEMBL3144849 — — 1 9.77
CHEMBL3144841 — — 1 9.70
CHEMBL19732 CGS-8216 — 1 9.60
CHEMBL133049 — — 1 9.54
CHEMBL6597 Ro-154513 — 1 9.52
CHEMBL341398 — — 1 9.52
CHEMBL6421 — — 1 9.52
CHEMBL3144753 — — 1 9.49
CHEMBL336728 — — 1 9.43
CHEMBL6659 — — 1 9.42
CHEMBL133272 — — 1 9.40
CHEMBL58757 — — 1 9.40
CHEMBL267665 RO-147437 — 1 9.40
CHEMBL3144615 — — 1 9.36
CHEMBL52030 — — 1 9.35
CHEMBL6655 — — 1 9.33
CHEMBL286594 — — 1 9.31
CHEMBL366947 BRETAZENIL 2.0 1 9.30
CHEMBL3144610 — — 1 9.28
CHEMBL407 FLUMAZENIL 4.0 1 9.22
CHEMBL415293 — — 1 9.19
CHEMBL133219 — — 1 9.15
CHEMBL339165 — — 1 9.11
CHEMBL3144617 — — 1 9.08
CHEMBL415290 Ro-151310 — 1 9.07
CHEMBL173329 — — 1 9.00
CHEMBL336377 — — 1 9.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3144696 — Ki = 0.08 nM 10.10
CHEMBL3144697 — Ki = 0.12 nM 9.92
CHEMBL130609 — Ki = 0.14 nM 9.85
CHEMBL3144849 — Ki = 0.17 nM 9.77
CHEMBL3144841 — Ki = 0.2 nM 9.70
CHEMBL19732 CGS-8216 Ki = 0.25 nM 9.60
CHEMBL133049 — Ki = 0.29 nM 9.54
CHEMBL6597 Ro-154513 Ki = 0.3 nM 9.52
CHEMBL6421 — Ki = 0.3 nM 9.52
CHEMBL341398 — Ki = 0.3 nM 9.52
CHEMBL3144753 — Ki = 0.32 nM 9.49
CHEMBL336728 — Ki = 0.37 nM 9.43
CHEMBL6659 — Ki = 0.38 nM 9.42
CHEMBL58757 — Ki = 0.4 nM 9.40
CHEMBL133272 — Ki = 0.4 nM 9.40
CHEMBL267665 RO-147437 Ki = 0.4 nM 9.40
CHEMBL3144615 — Ki = 0.44 nM 9.36
CHEMBL52030 — Ki = 0.45 nM 9.35
CHEMBL6655 — Ki = 0.47 nM 9.33
CHEMBL286594 — Ki = 0.49 nM 9.31
CHEMBL366947 BRETAZENIL Ki = 0.5 nM 9.30
CHEMBL3144610 — Ki = 0.52 nM 9.28
CHEMBL407 FLUMAZENIL Ki = 0.6 nM 9.22
CHEMBL415293 — Ki = 0.65 nM 9.19
CHEMBL133219 — Ki = 0.7 nM 9.15
CHEMBL339165 — Ki = 0.78 nM 9.11
CHEMBL3144617 — Ki = 0.84 nM 9.08
CHEMBL415290 Ro-151310 Ki = 0.85 nM 9.07
CHEMBL173329 — Ki = 1.0 nM 9.00
CHEMBL336377 — Ki = 1.0 nM 9.00
CHEMBL17468 — Ki = 1.04 nM 8.98
CHEMBL416450 — Ki = 1.07 nM 8.97
CHEMBL57655 — Ki = 1.1 nM 8.96
CHEMBL3144698 — Ki = 1.3 nM 8.89
CHEMBL339163 — Ki = 1.3 nM 8.89
CHEMBL58385 — Ki = 1.5 nM 8.82
CHEMBL646 TRIAZOLAM Ki = 1.54 nM 8.81
CHEMBL307202 — Ki = 1.54 nM 8.81
CHEMBL173082 — Ki = 1.6 nM 8.80
CHEMBL59180 — Ki = 1.68 nM 8.78
CHEMBL58570 — Ki = 1.72 nM 8.76
CHEMBL13280 FLUNITRAZEPAM Ki = 2.1 nM 8.68
CHEMBL134175 — Ki = 2.4 nM 8.62
CHEMBL49141 — Ki = 2.39 nM 8.62
CHEMBL6814 — Ki = 2.5 nM 8.60
CHEMBL130416 — Ki = 2.6 nM 8.59
CHEMBL300840 — Ki = 2.61 nM 8.58
CHEMBL85861 — Ki = 3.3 nM 8.48
CHEMBL7290 — Ki = 3.5 nM 8.46
CHEMBL336636 — Ki = 3.7 nM 8.43