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Assay Detail

CHEMBL747358

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

Binding
Displacement of [3H]ifenprodil binding to recombinant human NR1a/NR2B receptors expressed in L(tk-) cells
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

Novel N1-(benzyl)cinnamamidine derived NR2B subtype-selective NMDA receptor antagonists.
Curtis NR, Diggle HJ, Kulagowski JJ, London C, Grimwood S, Hutson PH, Murray F, Richards P, Macaulay A, Wafford KA.
Bioorg Med Chem Lett (2003) 13 : 693 -696
PubMed 12639560 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 31 7.95 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL423244 1 9.30
CHEMBL159675 1 9.22
CHEMBL158737 1 9.15
CHEMBL159762 1 9.10
CHEMBL159761 1 9.00
CHEMBL159416 1 8.89
CHEMBL159902 1 8.85
CHEMBL159453 1 8.85
CHEMBL159790 1 8.80
CHEMBL160027 1 8.77
CHEMBL161859 1 8.72
CHEMBL159425 1 8.57
CHEMBL350614 1 8.44
CHEMBL348727 1 8.24
CHEMBL159306 1 8.14
CHEMBL158874 1 8.05
CHEMBL305195 1 8.00
CHEMBL17350 TRAXOPRODIL 2.0 1 7.96
CHEMBL159894 1 7.92
CHEMBL161225 1 7.72
CHEMBL158510 1 7.51
CHEMBL161772 1 7.50
CHEMBL161332 1 7.28
CHEMBL162415 1 7.26
CHEMBL161008 1 7.11
CHEMBL353131 1 7.03
CHEMBL347424 1 7.01
CHEMBL161388 1 6.92
CHEMBL345169 1 6.28
CHEMBL159541 1 5.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL423244 Ki = 0.5 nM 9.30
CHEMBL159675 Ki = 0.6 nM 9.22
CHEMBL158737 Ki = 0.7 nM 9.15
CHEMBL159762 Ki = 0.8 nM 9.10
CHEMBL159761 Ki = 1.0 nM 9.00
CHEMBL159416 Ki = 1.3 nM 8.89
CHEMBL159902 Ki = 1.4 nM 8.85
CHEMBL159453 Ki = 1.4 nM 8.85
CHEMBL159790 Ki = 1.6 nM 8.80
CHEMBL160027 Ki = 1.7 nM 8.77
CHEMBL161859 Ki = 1.9 nM 8.72
CHEMBL159425 Ki = 2.7 nM 8.57
CHEMBL350614 Ki = 3.6 nM 8.44
CHEMBL348727 Ki = 5.7 nM 8.24
CHEMBL159306 Ki = 7.3 nM 8.14
CHEMBL158874 Ki = 9.0 nM 8.05
CHEMBL305195 Ki = 10.0 nM 8.00
CHEMBL17350 TRAXOPRODIL Ki = 11.0 nM 7.96
CHEMBL159894 Ki = 12.0 nM 7.92
CHEMBL161225 Ki = 19.0 nM 7.72
CHEMBL158510 Ki = 31.0 nM 7.51
CHEMBL161772 Ki = 32.0 nM 7.50
CHEMBL161332 Ki = 52.0 nM 7.28
CHEMBL162415 Ki = 55.0 nM 7.26
CHEMBL161008 Ki = 77.0 nM 7.11
CHEMBL353131 Ki = 93.0 nM 7.03
CHEMBL347424 Ki = 97.0 nM 7.01
CHEMBL161388 Ki = 120.0 nM 6.92
CHEMBL345169 Ki = 530.0 nM 6.28
CHEMBL159541 Ki = 1400.0 nM 5.85
CHEMBL350615 Ki = 10000.0 nM 5.00