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Assay Detail

CHEMBL674498

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

Binding
Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HEK293
Confidence 8 — Homologous single protein target
Curated By Expert

Target

D(4) dopamine receptor (CHEMBL219)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

4-N-linked-heterocyclic piperidine derivatives with high affinity and selectivity for human dopamine D4 receptors.
Moore KW, Bonner K, Jones EA, Emms F, Leeson PD, Marwood R, Patel S, Patel S, Rowley M, Thomas S, Carling RW.
Bioorg Med Chem Lett (1999) 9 : 1285 -1290
PubMed 10340615 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 7.95 9.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL279247 1 9.41
CHEMBL26120 1 8.92
CHEMBL25772 1 8.60
CHEMBL287412 1 8.51
CHEMBL24051 1 8.51
CHEMBL281195 1 8.33
CHEMBL24052 1 8.28
CHEMBL42 CLOZAPINE 4.0 1 8.00
CHEMBL25938 1 7.96
CHEMBL23537 1 7.82
CHEMBL284346 1 7.77
CHEMBL25887 1 7.75
CHEMBL24539 1 7.57
CHEMBL24170 1 7.50
CHEMBL287217 1 7.40
CHEMBL24809 1 6.85
CHEMBL24603 1 5.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL279247 Ki = 0.39 nM 9.41
CHEMBL26120 Ki = 1.2 nM 8.92
CHEMBL25772 Ki = 2.5 nM 8.60
CHEMBL287412 Ki = 3.1 nM 8.51
CHEMBL24051 Ki = 3.1 nM 8.51
CHEMBL281195 Ki = 4.7 nM 8.33
CHEMBL24052 Ki = 5.2 nM 8.28
CHEMBL42 CLOZAPINE Ki = 10.0 nM 8.00
CHEMBL25938 Ki = 11.0 nM 7.96
CHEMBL23537 Ki = 15.0 nM 7.82
CHEMBL284346 Ki = 17.0 nM 7.77
CHEMBL25887 Ki = 18.0 nM 7.75
CHEMBL24539 Ki = 27.0 nM 7.57
CHEMBL24170 Ki = 32.0 nM 7.50
CHEMBL287217 Ki = 40.0 nM 7.40
CHEMBL24809 Ki = 140.0 nM 6.85
CHEMBL24603 Ki = 1200.0 nM 5.92