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Assay Detail

CHEMBL747013

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

Binding
Binding affinity towards N-methyl-D-aspartate glutamate receptor 1 in rat cortical membranes using [3H]glycine as radioligand
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Glutamate receptor ionotropic, NMDA 1 (CHEMBL330)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

4,5-Dihydro-1,2,4-triazolo[1,5-a]quinoxalin-4-ones: excitatory amino acid antagonists with combined glycine/NMDA and AMPA receptor affinity.
Catarzi D, Colotta V, Varano F, Cecchi L, Filacchioni G, Galli A, Costagli C.
J Med Chem (1999) 42 : 2478 -2484
PubMed 10395489 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 28 5.44 6.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL311221 1 6.85
CHEMBL83551 1 6.77
CHEMBL82050 1 6.41
CHEMBL84283 1 6.24
CHEMBL420392 1 6.15
CHEMBL81874 1 6.15
CHEMBL310352 1 5.96
CHEMBL309441 1 5.96
CHEMBL79556 1 5.75
CHEMBL310014 1 5.66
CHEMBL81025 1 5.58
CHEMBL83919 1 5.52
CHEMBL79312 1 5.46
CHEMBL83322 1 5.35
CHEMBL309548 1 5.32
CHEMBL81367 1 5.29
CHEMBL83901 1 5.27
CHEMBL82684 1 5.19
CHEMBL82295 1 5.14
CHEMBL309206 1 5.12
CHEMBL313269 1 5.06
CHEMBL84094 1 5.01
CHEMBL86164 1 4.78
CHEMBL83902 1 4.56
CHEMBL311860 1 4.10
CHEMBL315484 1 4.06
CHEMBL83855 1 4.05
CHEMBL310544 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL311221 Ki = 140.0 nM 6.85
CHEMBL83551 Ki = 170.0 nM 6.77
CHEMBL82050 Ki = 390.0 nM 6.41
CHEMBL84283 Ki = 570.0 nM 6.24
CHEMBL420392 Ki = 710.0 nM 6.15
CHEMBL81874 Ki = 710.0 nM 6.15
CHEMBL310352 Ki = 1100.0 nM 5.96
CHEMBL309441 Ki = 1100.0 nM 5.96
CHEMBL79556 Ki = 1800.0 nM 5.75
CHEMBL310014 Ki = 2200.0 nM 5.66
CHEMBL81025 Ki = 2600.0 nM 5.58
CHEMBL83919 Ki = 3000.0 nM 5.52
CHEMBL79312 Ki = 3500.0 nM 5.46
CHEMBL83322 Ki = 4500.0 nM 5.35
CHEMBL309548 Ki = 4800.0 nM 5.32
CHEMBL81367 Ki = 5100.0 nM 5.29
CHEMBL83901 Ki = 5400.0 nM 5.27
CHEMBL82684 Ki = 6500.0 nM 5.19
CHEMBL82295 Ki = 7200.0 nM 5.14
CHEMBL309206 Ki = 7500.0 nM 5.12
CHEMBL313269 Ki = 8800.0 nM 5.06
CHEMBL84094 Ki = 9700.0 nM 5.01
CHEMBL86164 Ki = 16700.0 nM 4.78
CHEMBL83902 Ki = 27700.0 nM 4.56
CHEMBL311860 Ki = 79400.0 nM 4.10
CHEMBL315484 Ki = 88000.0 nM 4.06
CHEMBL83855 Ki = 88200.0 nM 4.05
CHEMBL310544 Ki > 100000.0 nM -