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Assay Detail

CHEMBL5527104

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Binding
Binding affinity to D1 receptor (unknown origin) assessed as inhibition constant
25
Total Activities
25
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(1A) dopamine receptor (CHEMBL2056)
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 25 7.04 9.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1672309 1 9.27
CHEMBL1672312 1 9.08
CHEMBL298406 ECOPIPAM 3.0 1 8.92
CHEMBL487387 STEPHOLIDINE 1 8.29
CHEMBL2334891 1 8.26
CHEMBL1962947 1 8.24
CHEMBL3697617 TAVAPADON 3.0 1 8.07
CHEMBL5563974 1 8.06
CHEMBL4633772 1 7.24
CHEMBL157138 LISURIDE 3.0 1 7.21
CHEMBL54 HALOPERIDOL 4.0 1 6.92
CHEMBL487182 TETRAHYDROPALMATINE 2.0 1 6.91
CHEMBL726 FLUPHENAZINE 4.0 1 6.75
CHEMBL4637246 1 6.52
CHEMBL1621 PALIPERIDONE 4.0 1 6.26
CHEMBL27559 1 6.16
CHEMBL225230 R-N-PROPYLNORAPOMORPHINE 1 6.13
CHEMBL531 PERGOLIDE 4.0 1 5.93
CHEMBL405345 1 5.77
CHEMBL59 DOPAMINE 4.0 1 5.63
CHEMBL493 BROMOCRIPTINE 4.0 1 5.47
CHEMBL2425376 1 5.42
CHEMBL1201087 CABERGOLINE 4.0 1 5.42
CHEMBL255229 1 -
CHEMBL403550 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1672309 Ki = 0.54 nM 9.27
CHEMBL1672312 Ki = 0.83 nM 9.08
CHEMBL298406 ECOPIPAM Ki = 1.2 nM 8.92
CHEMBL487387 STEPHOLIDINE Ki = 5.1 nM 8.29
CHEMBL2334891 Ki = 5.5 nM 8.26
CHEMBL1962947 Ki = 5.77 nM 8.24
CHEMBL3697617 TAVAPADON Ki = 8.54 nM 8.07
CHEMBL5563974 Ki = 8.75 nM 8.06
CHEMBL4633772 Ki = 58.0 nM 7.24
CHEMBL157138 LISURIDE Ki = 62.0 nM 7.21
CHEMBL54 HALOPERIDOL Ki = 120.0 nM 6.92
CHEMBL487182 TETRAHYDROPALMATINE Ki = 124.0 nM 6.91
CHEMBL726 FLUPHENAZINE Ki = 179.0 nM 6.75
CHEMBL4637246 Ki = 301.0 nM 6.52
CHEMBL1621 PALIPERIDONE Ki = 554.0 nM 6.26
CHEMBL27559 Ki = 699.0 nM 6.16
CHEMBL225230 R-N-PROPYLNORAPOMORPHINE Ki = 733.0 nM 6.13
CHEMBL531 PERGOLIDE Ki = 1163.0 nM 5.93
CHEMBL405345 Ki = 1690.0 nM 5.77
CHEMBL59 DOPAMINE Ki = 2340.0 nM 5.63
CHEMBL493 BROMOCRIPTINE Ki = 3418.0 nM 5.47
CHEMBL2425376 Ki = 3800.0 nM 5.42
CHEMBL1201087 CABERGOLINE Ki = 3800.0 nM 5.42
CHEMBL255229 Ki > 10000.0 nM -
CHEMBL403550 Ki > 20000.0 nM -