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Assay Detail

CHEMBL752567

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

Binding
Compound was evaluated for in vitro inhibition of [3H][(E)-N-(2-methoxybenzyl)cinnamamidine binding to human NR1a/NR2B receptors expressed in LtK-cells
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Glutamate NMDA receptor; GRIN1/GRIN2B (CHEMBL1907603)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

NR2B-selective N-methyl-D-aspartate antagonists: synthesis and evaluation of 5-substituted benzimidazoles.
McCauley JA, Theberge CR, Romano JJ, Billings SB, Anderson KD, Claremon DA, Freidinger RM, Bednar RA, Mosser SD, Gaul SL, Connolly TM, Condra CL, Xia M, Cunningham ME, Bednar B, Stump GL, Lynch JJ, Macaulay A, Wafford KA, Koblan KS, Liverton NJ.
J Med Chem (2004) 47 : 2089 -2096
PubMed 15056006 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 7.62 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL416690 1 9.40
CHEMBL65693 1 9.17
CHEMBL65454 1 9.09
CHEMBL68134 1 9.07
CHEMBL436521 1 9.00
CHEMBL64941 1 8.96
CHEMBL65231 1 8.82
CHEMBL65314 1 8.52
CHEMBL63200 1 8.49
CHEMBL303832 1 8.38
CHEMBL304274 1 7.82
CHEMBL66539 1 7.77
CHEMBL63992 1 7.68
CHEMBL65245 1 7.03
CHEMBL63924 1 6.85
CHEMBL65119 1 6.75
CHEMBL65039 1 6.62
CHEMBL67249 1 6.58
CHEMBL304070 1 6.38
CHEMBL61895 1 6.33
CHEMBL63474 1 6.10
CHEMBL63146 1 5.27
CHEMBL67196 1 5.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL416690 Ki = 0.4 nM 9.40
CHEMBL65693 Ki = 0.68 nM 9.17
CHEMBL65454 Ki = 0.82 nM 9.09
CHEMBL68134 Ki = 0.85 nM 9.07
CHEMBL436521 Ki = 0.99 nM 9.00
CHEMBL64941 Ki = 1.1 nM 8.96
CHEMBL65231 Ki = 1.5 nM 8.82
CHEMBL65314 Ki = 3.0 nM 8.52
CHEMBL63200 Ki = 3.2 nM 8.49
CHEMBL303832 Ki = 4.2 nM 8.38
CHEMBL304274 Ki = 15.0 nM 7.82
CHEMBL66539 Ki = 17.0 nM 7.77
CHEMBL63992 Ki = 21.0 nM 7.68
CHEMBL65245 Ki = 93.0 nM 7.03
CHEMBL63924 Ki = 140.0 nM 6.85
CHEMBL65119 Ki = 180.0 nM 6.75
CHEMBL65039 Ki = 240.0 nM 6.62
CHEMBL67249 Ki = 260.0 nM 6.58
CHEMBL304070 Ki = 420.0 nM 6.38
CHEMBL61895 Ki = 470.0 nM 6.33
CHEMBL63474 Ki = 790.0 nM 6.10
CHEMBL63146 Ki = 5400.0 nM 5.27
CHEMBL67196 Ki = 8400.0 nM 5.08