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Assay Detail

CHEMBL829006

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

Binding
Inhibition of [3H]Ro-151788 binding to recombinant human gamma-aminobutyric-acid A receptor alpha-1-beta-3-gamma-2 subtype expressed in L (tk-) cells
ChEMBL ↗
101
Total Activities
100
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-1/beta-3/gamma-2 (CHEMBL2094121) ↗
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Discovery of functionally selective 7,8,9,10-tetrahydro-7,10-ethano-1,2,4-triazolo[3,4-a]phthalazines as GABA A receptor agonists at the alpha3 subunit.
Russell MG, Carling RW, Atack JR, Bromidge FA, Cook SM, Hunt P, Isted C, Lucas M, McKernan RM, Mitchinson A, Moore KW, Narquizian R, Macaulay AJ, Thomas D, Thompson SA, Wafford KA, Castro JL.
J Med Chem (2005) 48 : 1367 -1383
PubMed 15743180 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 101 7.19 9.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL361114 — — 1 9.09
CHEMBL361129 — — 1 9.05
CHEMBL360122 — — 1 8.48
CHEMBL178677 — — 1 8.47
CHEMBL362485 — — 1 8.46
CHEMBL179414 — — 1 8.41
CHEMBL179558 — — 1 8.16
CHEMBL179474 — — 1 8.01
CHEMBL179712 — — 1 7.96
CHEMBL361786 — — 1 7.96
CHEMBL12 DIAZEPAM 4.0 1 7.89
CHEMBL179475 — — 1 7.89
CHEMBL175475 — — 1 7.89
CHEMBL178956 — — 1 7.80
CHEMBL180416 — — 1 7.77
CHEMBL366537 — — 1 7.72
CHEMBL359906 — — 1 7.68
CHEMBL359613 — — 1 7.68
CHEMBL179777 — — 1 7.66
CHEMBL362282 — — 1 7.64
CHEMBL911 ZOLPIDEM 4.0 1 7.57
CHEMBL369035 — — 1 7.57
CHEMBL178831 — — 1 7.55
CHEMBL178783 — — 1 7.54
CHEMBL366468 — — 1 7.51
CHEMBL180464 — — 1 7.50
CHEMBL180174 — — 1 7.48
CHEMBL359545 — — 1 7.46
CHEMBL359650 — — 1 7.37
CHEMBL175886 — — 1 7.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL361114 — Ki = 0.81 nM 9.09
CHEMBL361129 — Ki = 0.9 nM 9.05
CHEMBL360122 — Ki = 3.3 nM 8.48
CHEMBL178677 — Ki = 3.4 nM 8.47
CHEMBL362485 — Ki = 3.5 nM 8.46
CHEMBL179414 — Ki = 3.9 nM 8.41
CHEMBL179558 — Ki = 6.9 nM 8.16
CHEMBL179474 — Ki = 9.8 nM 8.01
CHEMBL179712 — Ki = 11.0 nM 7.96
CHEMBL361786 — Ki = 11.0 nM 7.96
CHEMBL12 DIAZEPAM Ki = 13.0 nM 7.89
CHEMBL179475 — Ki = 13.0 nM 7.89
CHEMBL175475 — Ki = 13.0 nM 7.89
CHEMBL178956 — Ki = 16.0 nM 7.80
CHEMBL180416 — Ki = 17.0 nM 7.77
CHEMBL366537 — Ki = 19.0 nM 7.72
CHEMBL359906 — Ki = 21.0 nM 7.68
CHEMBL359613 — Ki = 21.0 nM 7.68
CHEMBL179777 — Ki = 22.0 nM 7.66
CHEMBL362282 — Ki = 23.0 nM 7.64
CHEMBL911 ZOLPIDEM Ki = 27.0 nM 7.57
CHEMBL369035 — Ki = 27.0 nM 7.57
CHEMBL178831 — Ki = 28.0 nM 7.55
CHEMBL178783 — Ki = 29.0 nM 7.54
CHEMBL366468 — Ki = 31.0 nM 7.51
CHEMBL180464 — Ki = 32.0 nM 7.50
CHEMBL180174 — Ki = 33.0 nM 7.48
CHEMBL359545 — Ki = 35.0 nM 7.46
CHEMBL359650 — Ki = 43.0 nM 7.37
CHEMBL175886 — Ki = 50.0 nM 7.30
CHEMBL361340 — Ki = 53.0 nM 7.28
CHEMBL178710 — Ki = 56.0 nM 7.25
CHEMBL175929 — Ki = 60.0 nM 7.22
CHEMBL13662 CI-218872 Ki = 66.0 nM 7.18
CHEMBL360912 — Ki = 68.0 nM 7.17
CHEMBL178992 — Ki = 71.0 nM 7.15
CHEMBL178942 — Ki = 71.0 nM 7.15
CHEMBL362409 — Ki = 73.0 nM 7.14
CHEMBL180417 — Ki = 75.0 nM 7.12
CHEMBL179924 — Ki = 78.0 nM 7.11
CHEMBL440558 — Ki = 78.0 nM 7.11
CHEMBL366471 — Ki = 80.0 nM 7.10
CHEMBL361200 — Ki = 82.0 nM 7.09
CHEMBL361015 — Ki = 85.0 nM 7.07
CHEMBL361597 — Ki = 87.0 nM 7.06
CHEMBL360733 — Ki = 93.0 nM 7.03
CHEMBL178840 — Ki = 96.0 nM 7.02
CHEMBL179699 — Ki = 100.0 nM 7.00
CHEMBL362620 — Ki = 100.0 nM 7.00
CHEMBL178856 — Ki = 130.0 nM 6.89