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Assay Detail

CHEMBL745941

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

Functional
N-methyl-D-aspartate glutamate receptor antagonistic activity in cell culture(CC)model
18
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Glutamate NMDA receptor (CHEMBL1907608)
Type PROTEIN COMPLEX GROUP
Organism Rattus norvegicus

Publication

Separation of alpha 1 adrenergic and N-methyl-D-aspartate antagonist activity in a series of ifenprodil compounds.
Chenard BL, Shalaby IA, Koe BK, Ronau RT, Butler TW, Prochniak MA, Schmidt AW, Fox CB.
J Med Chem (1991) 34 : 3085 -3090
PubMed 1681106 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 6.40 7.88

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL319706 (S)-IFENPRODIL 3 7.88
CHEMBL323338 1 7.00
CHEMBL49623 (R,S)-IFENPRODIL 1 6.96
CHEMBL106970 1 6.82
CHEMBL104625 1 6.63
CHEMBL305187 IFENPRODIL 2.0 1 6.58
CHEMBL18222 1 6.54
CHEMBL102242 1 5.70
CHEMBL321349 1 5.43
CHEMBL106969 1 5.30
CHEMBL104363 1 5.20
CHEMBL262807 1 5.00
CHEMBL318347 1 -
CHEMBL322633 1 -
CHEMBL102212 1 -
CHEMBL104318 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL319706 (S)-IFENPRODIL IC50 = 13.3 nM 7.88
CHEMBL319706 (S)-IFENPRODIL IC50 = 48.0 nM 7.32
CHEMBL319706 (S)-IFENPRODIL IC50 = 55.0 nM 7.26
CHEMBL323338 IC50 = 100.0 nM 7.00
CHEMBL49623 (R,S)-IFENPRODIL IC50 = 110.0 nM 6.96
CHEMBL106970 IC50 = 153.0 nM 6.82
CHEMBL104625 IC50 = 233.0 nM 6.63
CHEMBL305187 IFENPRODIL IC50 = 263.0 nM 6.58
CHEMBL18222 IC50 = 290.0 nM 6.54
CHEMBL102242 IC50 = 2000.0 nM 5.70
CHEMBL321349 IC50 = 3700.0 nM 5.43
CHEMBL106969 IC50 = 5000.0 nM 5.30
CHEMBL104363 IC50 = 6300.0 nM 5.20
CHEMBL262807 IC50 = 10000.0 nM 5.00
CHEMBL102212 IC50 > 10000.0 nM -
CHEMBL322633 IC50 > 10000.0 nM -
CHEMBL318347 IC50 > 10000.0 nM -
CHEMBL104318 IC50 > 10000.0 nM -