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Assay Detail

CHEMBL5527107

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Binding
Binding affinity to D4 receptor (unknown origin) assessed as inhibition constant
9
Total Activities
9
Compounds Tested
1
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

Natural Product-Inspired Dopamine Receptor Ligands.
Dorogan M, Namballa HK, Harding WW.
J Med Chem (2024) 67 : 12463 -12484
PubMed 39038276 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 7.34 8.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL157138 LISURIDE 3.0 1 8.49
CHEMBL531 PERGOLIDE 4.0 1 8.21
CHEMBL59 DOPAMINE 4.0 1 8.19
CHEMBL54 HALOPERIDOL 4.0 1 7.52
CHEMBL1621 PALIPERIDONE 4.0 1 7.42
CHEMBL2334891 1 7.11
CHEMBL726 FLUPHENAZINE 4.0 1 6.89
CHEMBL493 BROMOCRIPTINE 4.0 1 6.43
CHEMBL487387 STEPHOLIDINE 1 5.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL157138 LISURIDE Ki = 3.2 nM 8.49
CHEMBL531 PERGOLIDE Ki = 6.2 nM 8.21
CHEMBL59 DOPAMINE Ki = 6.4 nM 8.19
CHEMBL54 HALOPERIDOL Ki = 30.3 nM 7.52
CHEMBL1621 PALIPERIDONE Ki = 38.0 nM 7.42
CHEMBL2334891 Ki = 77.4 nM 7.11
CHEMBL726 FLUPHENAZINE Ki = 130.0 nM 6.89
CHEMBL493 BROMOCRIPTINE Ki = 373.0 nM 6.43
CHEMBL487387 STEPHOLIDINE Ki = 1453.0 nM 5.84