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Assay Detail

CHEMBL675740

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

Binding
Displacement of [3H]- spiperone from dopamine receptor D2 of striatal membranes without sodium chloride
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Synthesis and in vitro evaluation of 2,3-dimethoxy-5-(fluoroalkyl)-substituted benzamides: high-affinity ligands for CNS dopamine D2 receptors.
Bishop JE, Mathis CA, Gerdes JM, Whitney JM, Eaton AM, Mailman RB.
J Med Chem (1991) 34 : 1612 -1624
PubMed 1827843 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 8.53 9.18

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL44237 EPIDEPRIDE 1 9.18
CHEMBL289330 1 9.12
CHEMBL43506 1 9.11
CHEMBL42448 1 9.10
CHEMBL8946 ETICLOPRIDE 2.0 1 9.00
CHEMBL42260 1 8.89
CHEMBL42953 1 8.36
CHEMBL288704 1 8.28
CHEMBL43552 1 8.16
CHEMBL8809 RACLOPRIDE 2.0 1 7.48
CHEMBL295621 1 7.18
CHEMBL2114460 1 -
CHEMBL2114461 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL44237 EPIDEPRIDE Ki = 0.66 nM 9.18
CHEMBL289330 Ki = 0.76 nM 9.12
CHEMBL43506 Ki = 0.77 nM 9.11
CHEMBL42448 Ki = 0.8 nM 9.10
CHEMBL8946 ETICLOPRIDE Ki = 0.99 nM 9.00
CHEMBL42260 Ki = 1.28 nM 8.89
CHEMBL42953 Ki = 4.4 nM 8.36
CHEMBL288704 Ki = 5.27 nM 8.28
CHEMBL43552 Ki = 6.98 nM 8.16
CHEMBL8809 RACLOPRIDE Ki = 32.8 nM 7.48
CHEMBL295621 Ki = 66.0 nM 7.18
CHEMBL2114460 Ki > 10000.0 nM -
CHEMBL2114461 Ki > 10000.0 nM -