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Assay Detail

CHEMBL5527105

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Binding
Binding affinity to D2 receptor (unknown origin) assessed as inhibition constant
20
Total Activities
20
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

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 20 7.61 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL157138 LISURIDE 3.0 1 9.52
CHEMBL1201087 CABERGOLINE 4.0 1 9.44
CHEMBL726 FLUPHENAZINE 4.0 1 8.84
CHEMBL1621 PALIPERIDONE 4.0 1 8.80
CHEMBL531 PERGOLIDE 4.0 1 8.40
CHEMBL225230 R-N-PROPYLNORAPOMORPHINE 1 8.00
CHEMBL493 BROMOCRIPTINE 4.0 1 8.00
CHEMBL54 HALOPERIDOL 4.0 1 7.98
CHEMBL487387 STEPHOLIDINE 1 7.94
CHEMBL59 DOPAMINE 4.0 1 7.90
CHEMBL27559 1 7.54
CHEMBL2334891 1 7.38
CHEMBL405345 1 7.36
CHEMBL255229 1 7.14
CHEMBL4637246 1 6.64
CHEMBL403550 1 6.47
CHEMBL487182 TETRAHYDROPALMATINE 2.0 1 6.41
CHEMBL1672309 1 6.31
CHEMBL1672312 1 6.12
CHEMBL4633772 1 6.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL157138 LISURIDE Ki = 0.3 nM 9.52
CHEMBL1201087 CABERGOLINE Ki = 0.36 nM 9.44
CHEMBL726 FLUPHENAZINE Ki = 1.44 nM 8.84
CHEMBL1621 PALIPERIDONE Ki = 1.6 nM 8.80
CHEMBL531 PERGOLIDE Ki = 4.0 nM 8.40
CHEMBL225230 R-N-PROPYLNORAPOMORPHINE Ki = 9.9 nM 8.00
CHEMBL493 BROMOCRIPTINE Ki = 10.0 nM 8.00
CHEMBL54 HALOPERIDOL Ki = 10.4 nM 7.98
CHEMBL487387 STEPHOLIDINE Ki = 11.6 nM 7.94
CHEMBL59 DOPAMINE Ki = 12.5 nM 7.90
CHEMBL27559 Ki = 28.5 nM 7.54
CHEMBL2334891 Ki = 41.8 nM 7.38
CHEMBL405345 Ki = 44.0 nM 7.36
CHEMBL255229 Ki = 72.3 nM 7.14
CHEMBL4637246 Ki = 231.0 nM 6.64
CHEMBL403550 Ki = 340.0 nM 6.47
CHEMBL487182 TETRAHYDROPALMATINE Ki = 388.0 nM 6.41
CHEMBL1672309 Ki = 490.0 nM 6.31
CHEMBL1672312 Ki = 750.0 nM 6.12
CHEMBL4633772 Ki = 854.0 nM 6.07