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Assay Detail

CHEMBL5527106

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Binding
Binding affinity to D3 receptor (unknown origin) assessed as inhibition constant
13
Total Activities
13
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(3) dopamine receptor (CHEMBL234)
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 13 7.50 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL157138 LISURIDE 3.0 1 8.77
CHEMBL59 DOPAMINE 4.0 1 8.52
CHEMBL726 FLUPHENAZINE 4.0 1 8.49
CHEMBL531 PERGOLIDE 4.0 1 8.40
CHEMBL1621 PALIPERIDONE 4.0 1 8.12
CHEMBL54 HALOPERIDOL 4.0 1 7.69
CHEMBL487387 STEPHOLIDINE 1 7.63
CHEMBL2334891 1 7.43
CHEMBL493 BROMOCRIPTINE 4.0 1 7.06
CHEMBL2425376 1 7.03
CHEMBL1962947 1 6.26
CHEMBL5563974 1 6.22
CHEMBL487182 TETRAHYDROPALMATINE 2.0 1 5.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL157138 LISURIDE Ki = 1.7 nM 8.77
CHEMBL59 DOPAMINE Ki = 3.0 nM 8.52
CHEMBL726 FLUPHENAZINE Ki = 3.2 nM 8.49
CHEMBL531 PERGOLIDE Ki = 4.0 nM 8.40
CHEMBL1621 PALIPERIDONE Ki = 7.5 nM 8.12
CHEMBL54 HALOPERIDOL Ki = 20.5 nM 7.69
CHEMBL487387 STEPHOLIDINE Ki = 23.4 nM 7.63
CHEMBL2334891 Ki = 37.3 nM 7.43
CHEMBL493 BROMOCRIPTINE Ki = 87.0 nM 7.06
CHEMBL2425376 Ki = 93.0 nM 7.03
CHEMBL1962947 Ki = 548.0 nM 6.26
CHEMBL5563974 Ki = 606.0 nM 6.22
CHEMBL487182 TETRAHYDROPALMATINE Ki = 1420.0 nM 5.85