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Assay Detail

CHEMBL4822010

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

Binding
Displacement of [3H]-methylspiperone from dopamine D4 receptor (unknown origin)
14
Total Activities
14
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

New tetrahydroisoquinoline-based D<sub>3</sub>R ligands with an o-xylenyl linker motif.
Cordone P, Namballa HK, Muniz B, Pal RK, Gallicchio E, Harding WW.
Bioorg Med Chem Lett (2021) 42 : 128047 -128047
PubMed 33882273 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 6.36 9.12
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL20734 NEMONAPRIDE 2.0 1 9.12
CHEMBL4846574 1 7.24
CHEMBL4876260 1 7.00
CHEMBL4878587 1 6.85
CHEMBL4856161 1 6.06
CHEMBL4878121 1 6.02
CHEMBL4854512 1 6.02
CHEMBL4857166 1 5.98
CHEMBL4867331 1 5.97
CHEMBL4862839 1 5.94
CHEMBL4876546 1 5.55
CHEMBL4877460 1 5.47
CHEMBL4863748 1 5.41
CHEMBL4854935 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL20734 NEMONAPRIDE Ki = 0.75 nM 9.12
CHEMBL4846574 Ki = 57.0 nM 7.24
CHEMBL4876260 Ki = 101.0 nM 7.00
CHEMBL4878587 Ki = 140.0 nM 6.85
CHEMBL4856161 Ki = 880.0 nM 6.06
CHEMBL4878121 Ki = 950.0 nM 6.02
CHEMBL4854512 Ki = 950.0 nM 6.02
CHEMBL4857166 Ki = 1040.0 nM 5.98
CHEMBL4867331 Ki = 1070.0 nM 5.97
CHEMBL4862839 Ki = 1150.0 nM 5.94
CHEMBL4876546 Ki = 2800.0 nM 5.55
CHEMBL4877460 Ki = 3360.0 nM 5.47
CHEMBL4863748 Ki = 3900.0 nM 5.41
CHEMBL4854935 Inhibition < 10.0 % -