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Assay Detail

CHEMBL780342

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

Functional
Compound was tested for neuroprotection against NMDA-Induced toxicity in cultured rat hippocampal neurons.
13
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 1 — Organism
Curated By Intermediate

Target

Rattus norvegicus (CHEMBL376)
Type ORGANISM
Organism Rattus norvegicus

Publication

(3R,4S)-3-[4-(4-fluorophenyl)-4-hydroxypiperidin-1-yl]chroman-4,7-diol: a conformationally restricted analogue of the NR2B subtype-selective NMDA antagonist (1S,2S)-1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidino)- 1-propanol.
Butler TW, Blake JF, Bordner J, Butler P, Chenard BL, Collins MA, DeCosta D, Ducat MJ, Eisenhard ME, Menniti FS, Pagnozzi MJ, Sands SB, Segelstein BE, Volberg W, White WF, Zhao D.
J Med Chem (1998) 41 : 1172 -1184
PubMed 9544217 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.31 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL17703 2 8.40
CHEMBL280083 2 8.05
CHEMBL17833 1 7.96
CHEMBL17885 1 7.70
CHEMBL277787 1 7.64
CHEMBL17595 1 7.60
CHEMBL417630 1 6.97
CHEMBL17909 1 6.80
CHEMBL17812 1 6.42
CHEMBL273354 1 6.27
CHEMBL17798 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL17703 IC50 = 4.0 nM 8.40
CHEMBL17703 IC50 = 5.0 nM 8.30
CHEMBL280083 IC50 = 9.0 nM 8.05
CHEMBL17833 IC50 = 11.0 nM 7.96
CHEMBL17885 IC50 = 20.0 nM 7.70
CHEMBL277787 IC50 = 23.0 nM 7.64
CHEMBL17595 IC50 = 25.0 nM 7.60
CHEMBL417630 IC50 = 108.0 nM 6.97
CHEMBL280083 IC50 = 129.0 nM 6.89
CHEMBL17909 IC50 = 160.0 nM 6.80
CHEMBL17812 IC50 = 383.0 nM 6.42
CHEMBL273354 IC50 = 533.0 nM 6.27
CHEMBL17798 IC50 = 1000.0 nM 6.00