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Assay Detail

CHEMBL887786

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

Binding
Binding affinity to NMDA NR2B receptor
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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
Ki 13 7.06 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL429656 1 8.70
CHEMBL393670 1 8.66
CHEMBL247323 1 8.44
CHEMBL247718 1 8.10
CHEMBL429475 1 7.18
CHEMBL159279 1 7.14
CHEMBL397784 1 7.12
CHEMBL247113 1 6.65
CHEMBL247717 1 6.53
CHEMBL247114 1 6.45
CHEMBL247115 1 6.30
CHEMBL391389 1 5.38
CHEMBL247716 1 5.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL429656 Ki = 2.0 nM 8.70
CHEMBL393670 Ki = 2.2 nM 8.66
CHEMBL247323 Ki = 3.6 nM 8.44
CHEMBL247718 Ki = 8.0 nM 8.10
CHEMBL429475 Ki = 66.0 nM 7.18
CHEMBL159279 Ki = 72.0 nM 7.14
CHEMBL397784 Ki = 75.0 nM 7.12
CHEMBL247113 Ki = 223.0 nM 6.65
CHEMBL247717 Ki = 296.0 nM 6.53
CHEMBL247114 Ki = 353.0 nM 6.45
CHEMBL247115 Ki = 505.0 nM 6.30
CHEMBL391389 Ki = 4197.0 nM 5.38
CHEMBL247716 Ki = 7350.0 nM 5.13