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Assay Detail

CHEMBL914284

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

Binding
Displacement of [3H]Ro 25,6981 from NR2B NMDA receptor in rat forebrain
57
Total Activities
57
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Glutamate receptor ionotropic, NMDA 2B (CHEMBL311)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Selective NR1/2B N-methyl-D-aspartate receptor antagonists among indole-2-carboxamides and benzimidazole-2-carboxamides.
Borza I, Bozó E, Barta-Szalai G, Kiss C, Tárkányi G, Demeter A, Gáti T, Háda V, Kolok S, Gere A, Fodor L, Nagy J, Galgóczy K, Magdó I, Agai B, Fetter J, Bertha F, Keserü GM, Horváth C, Farkas S, Greiner I, Domány G.
J Med Chem (2007) 50 : 901 -914
PubMed 17290978 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 57 7.65 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL222665 1 8.52
CHEMBL424752 1 8.52
CHEMBL219986 1 8.52
CHEMBL436521 1 8.46
CHEMBL220611 1 8.40
CHEMBL219631 BESONPRODIL -1.0 1 8.40
CHEMBL223248 1 8.40
CHEMBL222615 1 8.30
CHEMBL219987 1 8.30
CHEMBL220474 1 8.22
CHEMBL126929 1 8.22
CHEMBL374853 1 8.22
CHEMBL305195 1 8.22
CHEMBL17350 TRAXOPRODIL 2.0 1 8.15
CHEMBL127510 1 8.15
CHEMBL222197 1 8.05
CHEMBL375620 1 8.00
CHEMBL220041 1 8.00
CHEMBL373977 1 7.92
CHEMBL373891 1 7.92
CHEMBL333936 1 7.92
CHEMBL375615 1 7.85
CHEMBL374793 1 7.77
CHEMBL124873 1 7.75
CHEMBL374011 1 7.64
CHEMBL374676 1 7.55
CHEMBL126228 1 7.51
CHEMBL223695 1 7.51
CHEMBL419784 1 7.33
CHEMBL221108 1 7.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL222665 IC50 = 3.0 nM 8.52
CHEMBL219986 IC50 = 3.0 nM 8.52
CHEMBL424752 IC50 = 3.0 nM 8.52
CHEMBL436521 IC50 = 3.5 nM 8.46
CHEMBL220611 IC50 = 4.0 nM 8.40
CHEMBL219631 BESONPRODIL IC50 = 4.0 nM 8.40
CHEMBL223248 IC50 = 4.0 nM 8.40
CHEMBL222615 IC50 = 5.0 nM 8.30
CHEMBL219987 IC50 = 5.0 nM 8.30
CHEMBL220474 IC50 = 6.0 nM 8.22
CHEMBL126929 IC50 = 6.0 nM 8.22
CHEMBL374853 IC50 = 6.0 nM 8.22
CHEMBL305195 IC50 = 6.0 nM 8.22
CHEMBL127510 IC50 = 7.0 nM 8.15
CHEMBL17350 TRAXOPRODIL IC50 = 7.0 nM 8.15
CHEMBL222197 IC50 = 9.0 nM 8.05
CHEMBL375620 IC50 = 10.0 nM 8.00
CHEMBL220041 IC50 = 10.0 nM 8.00
CHEMBL373977 IC50 = 12.0 nM 7.92
CHEMBL373891 IC50 = 12.0 nM 7.92
CHEMBL333936 IC50 = 12.0 nM 7.92
CHEMBL375615 IC50 = 14.0 nM 7.85
CHEMBL374793 IC50 = 17.0 nM 7.77
CHEMBL124873 IC50 = 18.0 nM 7.75
CHEMBL374011 IC50 = 23.0 nM 7.64
CHEMBL374676 IC50 = 28.0 nM 7.55
CHEMBL223695 IC50 = 31.0 nM 7.51
CHEMBL126228 IC50 = 31.0 nM 7.51
CHEMBL419784 IC50 = 47.0 nM 7.33
CHEMBL221108 IC50 = 60.0 nM 7.22
CHEMBL375827 IC50 = 64.0 nM 7.19
CHEMBL426731 IC50 = 89.0 nM 7.05
CHEMBL124516 IC50 = 106.0 nM 6.97
CHEMBL374012 IC50 = 143.0 nM 6.84
CHEMBL373890 IC50 = 191.0 nM 6.72
CHEMBL113919 IC50 = 196.0 nM 6.71
CHEMBL220441 IC50 = 215.0 nM 6.67
CHEMBL339570 IC50 = 359.0 nM 6.45
CHEMBL123908 IC50 = 380.0 nM 6.42
CHEMBL220835 IC50 = 1084.0 nM 5.96
CHEMBL222457 IC50 = 1545.0 nM 5.81
CHEMBL222458 IC50 - -
CHEMBL375805 IC50 - -
CHEMBL221045 IC50 - -
CHEMBL220775 IC50 - -
CHEMBL220786 IC50 - -
CHEMBL220440 IC50 - -
CHEMBL219742 IC50 - -
CHEMBL338104 IC50 - -
CHEMBL221107 IC50 - -