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Assay Detail

CHEMBL798364

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

Functional
In vitro inhibition of glutamate induced neuronal death in primary cultures of rat hippocampal neurons.
21
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

(1S,2S)-1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidino)-1-propanol: a potent new neuroprotectant which blocks N-methyl-D-aspartate responses.
Chenard BL, Bordner J, Butler TW, Chambers LK, Collins MA, De Costa DL, Ducat MF, Dumont ML, Fox CB, Mena EE.
J Med Chem (1995) 38 : 3138 -3145
PubMed 7636876 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 7.41 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL420289 1 8.89
CHEMBL107075 1 8.70
CHEMBL107104 1 8.57
CHEMBL108120 1 8.40
CHEMBL17350 TRAXOPRODIL 2.0 2 7.99
CHEMBL321758 1 7.96
CHEMBL105870 1 7.80
CHEMBL319706 (S)-IFENPRODIL 1 7.26
CHEMBL107055 1 7.24
CHEMBL107148 1 7.20
CHEMBL104314 1 7.17
CHEMBL49623 (R,S)-IFENPRODIL 1 6.58
CHEMBL106191 1 6.00
CHEMBL321428 1 5.89
CHEMBL262807 1 5.00
CHEMBL102212 1 -
CHEMBL106650 1 -
CHEMBL431867 1 -
CHEMBL109121 1 -
CHEMBL107303 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL420289 IC50 = 1.3 nM 8.89
CHEMBL107075 IC50 = 2.0 nM 8.70
CHEMBL107104 IC50 = 2.7 nM 8.57
CHEMBL108120 IC50 = 4.0 nM 8.40
CHEMBL17350 TRAXOPRODIL IC50 = 10.2 nM 7.99
CHEMBL17350 TRAXOPRODIL IC50 = 11.0 nM 7.96
CHEMBL321758 IC50 = 11.0 nM 7.96
CHEMBL105870 IC50 = 15.7 nM 7.80
CHEMBL319706 (S)-IFENPRODIL IC50 = 55.0 nM 7.26
CHEMBL107055 IC50 = 58.0 nM 7.24
CHEMBL107148 IC50 = 63.0 nM 7.20
CHEMBL104314 IC50 = 68.0 nM 7.17
CHEMBL49623 (R,S)-IFENPRODIL IC50 = 263.0 nM 6.58
CHEMBL106191 IC50 = 1000.0 nM 6.00
CHEMBL321428 IC50 = 1300.0 nM 5.89
CHEMBL262807 IC50 = 10000.0 nM 5.00
CHEMBL102212 IC50 > 10000.0 nM -
CHEMBL106650 IC50 > 1000.0 nM -
CHEMBL431867 IC50 > 10000.0 nM -
CHEMBL109121 IC50 > 1000.0 nM -
CHEMBL107303 IC50 > 1000.0 nM -