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Assay Detail

CHEMBL872844

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

Binding
Evaluated for their affinity at the PCP site for displacement of [3H]TCP in rat brain homogenates
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and pharmacological evaluation of hexahydrofluorenamines as noncompetitive antagonists at the N-methyl-D-aspartate receptor.
Hays SJ, Novak PM, Ortwine DF, Bigge CF, Colbry NL, Johnson G, Lescosky LJ, Malone TC, Michael A, Reily MD.
J Med Chem (1993) 36 : 654 -670
PubMed 8459395 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 7.18 8.73

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL162352 1 8.73
CHEMBL284237 DIZOCILPINE 2.0 1 8.54
CHEMBL157931 1 8.00
CHEMBL435581 1 7.95
CHEMBL158523 1 7.87
CHEMBL349923 1 7.78
CHEMBL351301 1 7.66
CHEMBL1795070 1 7.52
CHEMBL275528 PHENCYCLIDINE 2.0 1 7.44
CHEMBL145350 1 7.26
CHEMBL347859 1 7.18
CHEMBL160716 1 7.10
CHEMBL349852 1 7.02
CHEMBL158675 1 6.97
CHEMBL305904 ETOXADROL 2.0 1 6.97
CHEMBL158540 1 6.95
CHEMBL158858 1 6.85
CHEMBL349315 1 6.80
CHEMBL349819 1 6.60
CHEMBL159154 1 6.52
CHEMBL160855 1 6.49
CHEMBL348500 1 6.46
CHEMBL159098 1 6.28
CHEMBL161405 1 5.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL162352 IC50 = 1.84 nM 8.73
CHEMBL284237 DIZOCILPINE IC50 = 2.92 nM 8.54
CHEMBL157931 IC50 = 9.9 nM 8.00
CHEMBL435581 IC50 = 11.3 nM 7.95
CHEMBL158523 IC50 = 13.4 nM 7.87
CHEMBL349923 IC50 = 16.5 nM 7.78
CHEMBL351301 IC50 = 22.0 nM 7.66
CHEMBL1795070 IC50 = 30.0 nM 7.52
CHEMBL275528 PHENCYCLIDINE IC50 = 36.5 nM 7.44
CHEMBL145350 IC50 = 55.2 nM 7.26
CHEMBL347859 IC50 = 66.0 nM 7.18
CHEMBL160716 IC50 = 79.0 nM 7.10
CHEMBL349852 IC50 = 95.0 nM 7.02
CHEMBL158675 IC50 = 107.0 nM 6.97
CHEMBL305904 ETOXADROL IC50 = 107.0 nM 6.97
CHEMBL158540 IC50 = 113.0 nM 6.95
CHEMBL158858 IC50 = 141.0 nM 6.85
CHEMBL349315 IC50 = 159.0 nM 6.80
CHEMBL349819 IC50 = 253.0 nM 6.60
CHEMBL159154 IC50 = 304.0 nM 6.52
CHEMBL160855 IC50 = 323.0 nM 6.49
CHEMBL348500 IC50 = 350.0 nM 6.46
CHEMBL159098 IC50 = 528.0 nM 6.28
CHEMBL161405 IC50 = 3935.0 nM 5.41