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Assay Detail

CHEMBL675896

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Binding
Binding affinity towards cloned human Dopamine receptor D3 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Expert

Target

D(3) dopamine receptor (CHEMBL234)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

3-((4-(4-Chlorophenyl)piperazin-1-yl)-methyl)-1H-pyrrolo-2,3-b-pyridine: an antagonist with high affinity and selectivity for the human dopamine D4 receptor.
Kulagowski JJ, Broughton HB, Curtis NR, Mawer IM, Ridgill MP, Baker R, Emms F, Freedman SB, Marwood R, Patel S, Patel S, Ragan CI, Leeson PD.
J Med Chem (1996) 39 : 1941 -1942
PubMed 8642550 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 6.70 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 8.70
CHEMBL59103 1 7.02
CHEMBL445102 1 7.00
CHEMBL268799 1 6.82
CHEMBL42 CLOZAPINE 4.0 1 6.70
CHEMBL59324 1 6.55
CHEMBL267014 L-745870 1 5.64
CHEMBL57478 1 5.17
CHEMBL60518 1 -
CHEMBL57535 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 2.0 nM 8.70
CHEMBL59103 Ki = 95.0 nM 7.02
CHEMBL445102 Ki = 100.0 nM 7.00
CHEMBL268799 Ki = 150.0 nM 6.82
CHEMBL42 CLOZAPINE Ki = 200.0 nM 6.70
CHEMBL59324 Ki = 280.0 nM 6.55
CHEMBL267014 L-745870 Ki = 2300.0 nM 5.64
CHEMBL57478 Ki = 6700.0 nM 5.17
CHEMBL60518 Ki > 4500.0 nM -
CHEMBL57535 Ki > 3700.0 nM -