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Assay Detail

CHEMBL4628381

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Binding
Binding affinity to human D2 receptor
12
Total Activities
12
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(2) dopamine receptor (CHEMBL217)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of C10 nitrogen-containing aporphines with dopamine D<sub>1</sub> versus D<sub>5</sub> receptor selectivity.
Karki A, Juarez R, Namballa HK, Alberts I, Harding WW.
Bioorg Med Chem Lett (2020) 30 : 127053 -127053
PubMed 32107165 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 6.43 8.71

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 8.71
CHEMBL4637246 1 6.64
CHEMBL4639398 1 6.58
CHEMBL4636948 1 6.50
CHEMBL4636589 1 6.37
CHEMBL4646927 1 6.32
CHEMBL4634039 1 6.17
CHEMBL4649785 1 6.12
CHEMBL4633772 1 6.07
CHEMBL4636318 1 6.02
CHEMBL4637673 1 6.01
CHEMBL4638749 1 5.69

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 1.97 nM 8.71
CHEMBL4637246 Ki = 231.0 nM 6.64
CHEMBL4639398 Ki = 260.0 nM 6.58
CHEMBL4636948 Ki = 320.0 nM 6.50
CHEMBL4636589 Ki = 431.0 nM 6.37
CHEMBL4646927 Ki = 478.0 nM 6.32
CHEMBL4634039 Ki = 679.0 nM 6.17
CHEMBL4649785 Ki = 759.0 nM 6.12
CHEMBL4633772 Ki = 854.0 nM 6.07
CHEMBL4636318 Ki = 963.0 nM 6.02
CHEMBL4637673 Ki = 978.0 nM 6.01
CHEMBL4638749 Ki = 2048.0 nM 5.69