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Assay Detail

CHEMBL675767

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

Binding
Inhibition of [3H]-raclopride binding at Dopamine receptor D2 in rat brain membranes.
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Subcellular Brain membranes
Confidence 8 — Homologous single protein target
Curated By Expert

Target

D(2) dopamine receptor (CHEMBL339)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis of N-substituted 4-(4-hydroxyphenyl)piperidines, 4-(4-hydroxybenzyl)piperidines, and (+/-)-3-(4-hydroxyphenyl)pyrrolidines: selective antagonists at the 1A/2B NMDA receptor subtype.
Guzikowski AP, Tamiz AP, Acosta-Burruel M, Hong-Bae S, Cai SX, Hawkinson JE, Keana JF, Kesten SR, Shipp CT, Tran M, Whittemore ER, Woodward RM, Wright JL, Zhou ZL.
J Med Chem (2000) 43 : 984 -994
PubMed 10715162 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.55 6.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1203894 1 6.39
CHEMBL1202296 1 5.92
CHEMBL177620 1 5.23
CHEMBL174632 1 4.66
CHEMBL177624 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1203894 IC50 = 410.0 nM 6.39
CHEMBL1202296 IC50 = 1200.0 nM 5.92
CHEMBL177620 IC50 = 5900.0 nM 5.23
CHEMBL174632 IC50 = 22000.0 nM 4.66
CHEMBL177624 IC50 = 105000.0 nM -