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Assay Detail

CHEMBL4480642

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

Binding
Displacement of [3H]-ifenprodil from GluN2B (unknown origin) expressed in rat L(tk) cells measured after 120 mins by scintillation counting analysis
6
Total Activities
6
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

Synthesis and receptor binding of thiophene bioisosteres of potent GluN2B ligands with a benzo[7]annulene-scaffold.
Baumeister S, Schepmann D, Wünsch B.
Medchemcomm (2019) 10 : 315 -325
PubMed 30881618 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 7.38 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL305187 IFENPRODIL 2.0 1 8.00
CHEMBL4287203 1 7.80
CHEMBL4574247 1 7.58
CHEMBL4590193 1 7.32
CHEMBL4570472 1 6.89
CHEMBL4513837 1 6.69

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL305187 IFENPRODIL Ki = 10.0 nM 8.00
CHEMBL4287203 Ki = 16.0 nM 7.80
CHEMBL4574247 Ki = 26.0 nM 7.58
CHEMBL4590193 Ki = 48.0 nM 7.32
CHEMBL4570472 Ki = 128.0 nM 6.89
CHEMBL4513837 Ki = 204.0 nM 6.69