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Assay Detail

CHEMBL751683

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

Binding
Binding affinity against NMDA receptor by displacement of [3H]Ro-256981
29
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Glutamate [NMDA] receptor (CHEMBL2094124)
Type PROTEIN COMPLEX GROUP
Organism Homo sapiens

Publication

2-(3,4-Dihydro-1H-isoquinolin-2yl)-pyridines as a novel class of NR1/2B subtype selective NMDA receptor antagonists.
Büttelmann B, Alanine A, Bourson A, Gill R, Heitz MP, Mutel V, Pinard E, Trube G, Wyler R.
Bioorg Med Chem Lett (2003) 13 : 829 -832
PubMed 12617901 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 29 7.31 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL299294 1 8.70
CHEMBL166991 1 8.52
CHEMBL166935 1 8.52
CHEMBL50872 1 8.46
CHEMBL169695 1 8.40
CHEMBL170552 1 8.40
CHEMBL354482 1 8.40
CHEMBL166697 1 8.30
CHEMBL305195 1 8.22
CHEMBL168496 1 8.10
CHEMBL167004 1 8.10
CHEMBL166599 2 8.10
CHEMBL169469 1 8.05
CHEMBL17350 TRAXOPRODIL 2.0 1 7.96
CHEMBL49623 (R,S)-IFENPRODIL 1 7.89
CHEMBL168273 1 6.96
CHEMBL352819 1 6.82
CHEMBL168650 1 6.72
CHEMBL170163 1 6.58
CHEMBL168559 1 6.42
CHEMBL353194 1 6.42
CHEMBL167128 1 6.42
CHEMBL168262 1 6.12
CHEMBL168925 1 5.96
CHEMBL354066 1 5.96
CHEMBL169101 1 5.77
CHEMBL168488 1 5.12
CHEMBL170056 1 4.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL299294 Ki = 2.0 nM 8.70
CHEMBL166991 Ki = 3.0 nM 8.52
CHEMBL166935 Ki = 3.0 nM 8.52
CHEMBL50872 Ki = 3.5 nM 8.46
CHEMBL169695 Ki = 4.0 nM 8.40
CHEMBL170552 Ki = 4.0 nM 8.40
CHEMBL354482 Ki = 4.0 nM 8.40
CHEMBL166697 Ki = 5.0 nM 8.30
CHEMBL305195 Ki = 6.0 nM 8.22
CHEMBL168496 Ki = 8.0 nM 8.10
CHEMBL167004 Ki = 8.0 nM 8.10
CHEMBL166599 Ki = 8.0 nM 8.10
CHEMBL169469 Ki = 9.0 nM 8.05
CHEMBL17350 TRAXOPRODIL Ki = 11.0 nM 7.96
CHEMBL49623 (R,S)-IFENPRODIL Ki = 13.0 nM 7.89
CHEMBL166599 Ki = 19.0 nM 7.72
CHEMBL168273 Ki = 110.0 nM 6.96
CHEMBL352819 Ki = 150.0 nM 6.82
CHEMBL168650 Ki = 190.0 nM 6.72
CHEMBL170163 Ki = 260.0 nM 6.58
CHEMBL168559 Ki = 380.0 nM 6.42
CHEMBL353194 Ki = 380.0 nM 6.42
CHEMBL167128 Ki = 380.0 nM 6.42
CHEMBL168262 Ki = 750.0 nM 6.12
CHEMBL168925 Ki = 1100.0 nM 5.96
CHEMBL354066 Ki = 1100.0 nM 5.96
CHEMBL169101 Ki = 1700.0 nM 5.77
CHEMBL168488 Ki = 7500.0 nM 5.12
CHEMBL170056 Ki = 15000.0 nM 4.82