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Assay Detail

CHEMBL858425

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Binding
In vitro binding affinity for glycine site on the NMDA receptor.
34
Total Activities
33
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

Synthesis and biological evaluation of pyrido[2,3-b]pyrazine and pyrido[2,3-b]pyrazine-n-oxide as selective glycine antagonists
Cugola A, Donati D, Guarneri M, Micheli F, Missio A, Pecunioso A, Reggiani A, Tarzia G, Zanirato V
Bioorg Med Chem Lett (1996) 6 : 2749 -2754
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 34 6.18 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL316319 1 6.96
CHEMBL327343 1 6.95
CHEMBL328571 1 6.95
CHEMBL93473 2 6.84
CHEMBL93164 1 6.73
CHEMBL93165 1 6.72
CHEMBL90253 1 6.69
CHEMBL94018 1 6.68
CHEMBL91698 1 6.65
CHEMBL329176 1 6.55
CHEMBL330190 1 6.43
CHEMBL327178 1 6.37
CHEMBL91801 1 6.37
CHEMBL94925 1 6.34
CHEMBL92845 1 6.33
CHEMBL93837 1 6.30
CHEMBL96359 1 6.29
CHEMBL92456 1 6.29
CHEMBL92282 1 6.27
CHEMBL432648 1 6.13
CHEMBL93062 1 6.09
CHEMBL92143 1 6.04
CHEMBL96878 1 5.82
CHEMBL329680 1 5.80
CHEMBL92674 1 5.80
CHEMBL92080 1 5.75
CHEMBL424246 1 5.56
CHEMBL92084 1 5.54
CHEMBL327344 1 5.52
CHEMBL328357 1 5.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL316319 Ki = 109.65 nM 6.96
CHEMBL327343 Ki = 112.2 nM 6.95
CHEMBL328571 Ki = 112.2 nM 6.95
CHEMBL93473 Ki = 144.54 nM 6.84
CHEMBL93164 Ki = 186.21 nM 6.73
CHEMBL93165 Ki = 190.55 nM 6.72
CHEMBL90253 Ki = 204.17 nM 6.69
CHEMBL94018 Ki = 208.93 nM 6.68
CHEMBL91698 Ki = 223.87 nM 6.65
CHEMBL329176 Ki = 281.84 nM 6.55
CHEMBL330190 Ki = 371.54 nM 6.43
CHEMBL91801 Ki = 426.58 nM 6.37
CHEMBL327178 Ki = 426.58 nM 6.37
CHEMBL94925 Ki = 457.09 nM 6.34
CHEMBL92845 Ki = 467.74 nM 6.33
CHEMBL93837 Ki = 501.19 nM 6.30
CHEMBL92456 Ki = 512.86 nM 6.29
CHEMBL96359 Ki = 512.86 nM 6.29
CHEMBL92282 Ki = 537.03 nM 6.27
CHEMBL432648 Ki = 741.31 nM 6.13
CHEMBL93062 Ki = 812.83 nM 6.09
CHEMBL92143 Ki = 912.01 nM 6.04
CHEMBL96878 Ki = 1513.56 nM 5.82
CHEMBL329680 Ki = 1584.89 nM 5.80
CHEMBL92674 Ki = 1584.89 nM 5.80
CHEMBL92080 Ki = 1778.28 nM 5.75
CHEMBL93473 Ki = 1905.46 nM 5.72
CHEMBL424246 Ki = 2754.23 nM 5.56
CHEMBL92084 Ki = 2884.03 nM 5.54
CHEMBL327344 Ki = 3019.95 nM 5.52
CHEMBL328357 Ki = 3162.28 nM 5.50
CHEMBL92194 Ki = 3715.35 nM 5.43
CHEMBL92646 Ki = 4677.35 nM 5.33
CHEMBL27648 Ki = 6165.95 nM 5.21