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Assay Detail

CHEMBL887787

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Functional
Antagonist activity at NMDA NR2B receptor assessed as calcium flux
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Glutamate receptor ionotropic, NMDA 2B (CHEMBL1904)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Cyclic benzamidines as orally efficacious NR2B-selective NMDA receptor antagonists.
Nguyen KT, Claiborne CF, McCauley JA, Libby BE, Claremon DA, Bednar RA, Mosser SD, Gaul SL, Connolly TM, Condra CL, Bednar B, Stump GL, Lynch JJ, Koblan KS, Liverton NJ.
Bioorg Med Chem Lett (2007) 17 : 3997 -4000
PubMed 17498948 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.75 8.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL247323 1 8.23
CHEMBL393670 1 7.92
CHEMBL429656 1 7.41
CHEMBL159279 1 7.33
CHEMBL247718 1 7.31
CHEMBL397784 1 6.97
CHEMBL429475 1 6.58
CHEMBL247114 1 5.90
CHEMBL247717 1 5.70
CHEMBL247115 1 5.46
CHEMBL247113 1 5.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL247323 IC50 = 5.9 nM 8.23
CHEMBL393670 IC50 = 12.0 nM 7.92
CHEMBL429656 IC50 = 39.0 nM 7.41
CHEMBL159279 IC50 = 47.0 nM 7.33
CHEMBL247718 IC50 = 49.0 nM 7.31
CHEMBL397784 IC50 = 108.0 nM 6.97
CHEMBL429475 IC50 = 266.0 nM 6.58
CHEMBL247114 IC50 = 1270.0 nM 5.90
CHEMBL247717 IC50 = 1976.0 nM 5.70
CHEMBL247115 IC50 = 3480.0 nM 5.46
CHEMBL247113 IC50 = 3670.0 nM 5.43