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Assay Detail

CHEMBL978910

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

Binding
Displacement of [3H]MK801 from NMDA receptor in rat brain neuronal membrane
39
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

NMDA receptor affinities of 1,2-diphenylethylamine and 1-(1,2-diphenylethyl)piperidine enantiomers and of related compounds.
Berger ML, Schweifer A, Rebernik P, Hammerschmidt F.
Bioorg Med Chem (2009) 17 : 3456 -3462
PubMed 19345586 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 39 5.51 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL284237 DIZOCILPINE 2.0 2 8.05
CHEMBL467085 1 6.92
CHEMBL275528 PHENCYCLIDINE 2.0 1 6.57
CHEMBL449151 1 6.16
CHEMBL447983 1 6.10
CHEMBL395091 ESKETAMINE 4.0 1 6.02
CHEMBL1638 1 5.77
CHEMBL1908323 LEVOMETHORPHAN 2.0 1 5.47
CHEMBL467126 1 5.38
CHEMBL381340 1 5.38
CHEMBL52440 DEXTROMETHORPHAN 4.0 1 5.34
CHEMBL466089 1 5.28
CHEMBL467505 1 5.25
CHEMBL451286 1 5.09
CHEMBL467084 LANICEMINE 2.0 1 4.85
CHEMBL461517 1 4.80
CHEMBL467307 1 4.60
CHEMBL467308 1 4.29
CHEMBL467504 1 4.26
CHEMBL467503 AMINODIPHENYLMETHANE 1 4.19
CHEMBL466285 1 4.08
CHEMBL446225 1 -
CHEMBL19969 1 -
CHEMBL442934 1 -
CHEMBL612 DEXTROAMPHETAMINE 4.0 1 -
CHEMBL257990 (+)-TRANYLCYPROMINE 1 -
CHEMBL467523 1 -
CHEMBL467528 1 -
CHEMBL53697 1 -
CHEMBL10780 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL284237 DIZOCILPINE Ki = 9.0 nM 8.05
CHEMBL284237 DIZOCILPINE Ki = 43.0 nM 7.37
CHEMBL467085 Ki = 120.0 nM 6.92
CHEMBL275528 PHENCYCLIDINE Ki = 270.0 nM 6.57
CHEMBL449151 Ki = 700.0 nM 6.16
CHEMBL447983 Ki = 790.0 nM 6.10
CHEMBL395091 ESKETAMINE Ki = 960.0 nM 6.02
CHEMBL1638 Ki = 1700.0 nM 5.77
CHEMBL1908323 LEVOMETHORPHAN Ki = 3360.0 nM 5.47
CHEMBL467126 Ki = 4180.0 nM 5.38
CHEMBL381340 Ki = 4120.0 nM 5.38
CHEMBL52440 DEXTROMETHORPHAN Ki = 4540.0 nM 5.34
CHEMBL466089 Ki = 5250.0 nM 5.28
CHEMBL467505 Ki = 5680.0 nM 5.25
CHEMBL451286 Ki = 8080.0 nM 5.09
CHEMBL467084 LANICEMINE Ki = 14000.0 nM 4.85
CHEMBL461517 Ki = 15700.0 nM 4.80
CHEMBL467307 Ki = 25100.0 nM 4.60
CHEMBL467308 Ki = 51000.0 nM 4.29
CHEMBL467504 Ki = 55000.0 nM 4.26
CHEMBL467503 AMINODIPHENYLMETHANE Ki = 64000.0 nM 4.19
CHEMBL466285 Ki = 84000.0 nM 4.08
CHEMBL510603 Ki = 271000.0 nM -
CHEMBL522 BENZYLAMINE Ki = 1063000.0 nM -
CHEMBL610 PHENETHYLAMINE Ki = 753000.0 nM -
CHEMBL282700 Ki = 622000.0 nM -
CHEMBL19393 LEVAMFETAMINE Ki = 625000.0 nM -
CHEMBL3989843 TRANYLCYPROMINE Ki = 544000.0 nM -
CHEMBL502179 Ki = 1372000.0 nM -
CHEMBL51969 PHENYLALANINE METHYL ESTER Ki = 701000.0 nM -
CHEMBL10780 Ki = 145000.0 nM -
CHEMBL53697 Ki = 855000.0 nM -
CHEMBL467528 Ki - -
CHEMBL467523 Ki = 1978000.0 nM -
CHEMBL257990 (+)-TRANYLCYPROMINE Ki = 269000.0 nM -
CHEMBL612 DEXTROAMPHETAMINE Ki = 300000.0 nM -
CHEMBL19969 Ki = 659000.0 nM -
CHEMBL442934 Ki = 142000.0 nM -
CHEMBL446225 Ki = 138000.0 nM -