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Assay Detail

CHEMBL4182983

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

Binding
Displacement of [3H]-ifenprodil from recombinant human GluN1a/GluN2B expressed in L(tk-) cell membranes after 120 mins by scintillation counting analysis
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

2-Methyltetrahydro-3-benzazepin-1-ols - The missing link in SAR of GluN2B selective NMDA receptor antagonists.
Dey S, Schepmann D, Wünsch B.
Bioorg Med Chem (2018) 26 : 501 -508
PubMed 29254894 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 7.31 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL305187 IFENPRODIL 2.0 1 8.00
CHEMBL1289626 1 7.85
CHEMBL4206913 1 7.77
CHEMBL4218465 1 7.25
CHEMBL3753409 1 7.14
CHEMBL4204621 1 6.60
CHEMBL4205955 1 6.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL305187 IFENPRODIL Ki = 10.0 nM 8.00
CHEMBL1289626 Ki = 14.0 nM 7.85
CHEMBL4206913 Ki = 17.0 nM 7.77
CHEMBL4218465 Ki = 56.0 nM 7.25
CHEMBL3753409 Ki = 73.0 nM 7.14
CHEMBL4204621 Ki = 252.0 nM 6.60
CHEMBL4205955 Ki = 259.0 nM 6.59