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Assay Detail

CHEMBL749677

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

Binding
Displacement of racemic [3H]CP-101606 from rat forebrain membrane N-methyl-D-aspartate glutamate receptor 2B
12
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 12 7.36 7.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL277787 1 7.77
CHEMBL17703 2 7.75
CHEMBL17198 1 7.70
CHEMBL17350 TRAXOPRODIL 2.0 1 7.57
CHEMBL280083 2 7.51
CHEMBL17833 1 7.46
CHEMBL417630 1 6.97
CHEMBL17909 1 6.89
CHEMBL278666 1 6.52
CHEMBL17933 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL277787 IC50 = 17.0 nM 7.77
CHEMBL17703 IC50 = 18.0 nM 7.75
CHEMBL17198 IC50 = 20.0 nM 7.70
CHEMBL17350 TRAXOPRODIL IC50 = 27.0 nM 7.57
CHEMBL17703 IC50 = 28.0 nM 7.55
CHEMBL280083 IC50 = 31.0 nM 7.51
CHEMBL17833 IC50 = 35.0 nM 7.46
CHEMBL280083 IC50 = 54.0 nM 7.27
CHEMBL417630 IC50 = 107.0 nM 6.97
CHEMBL17909 IC50 = 130.0 nM 6.89
CHEMBL278666 IC50 = 300.0 nM 6.52
CHEMBL17933 IC50 > 300.0 nM -