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Assay Detail

CHEMBL4688550

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [3H]-N-methylspiperone from human dopamine D3 receptor by liquid scintillation counting
32
Total Activities
17
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

A study of the structure-affinity relationship in SYA16263; is a D receptor interaction essential for inhibition of apormorphine-induced climbing behavior in mice?
Onyameh EK,Bricker BA,Eyunni SVK,Voshavar C,Gonela UM,Ofori E,Jenkins A,Ablordeppey SY
Bioorg Med Chem (2021) 30 : 115943 -115943
PubMed 33338898 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 32 6.63 8.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1112 ARIPIPRAZOLE 4.0 1 8.01
CHEMBL4574793 2 7.58
CHEMBL4753809 2 7.27
CHEMBL4743284 2 7.24
CHEMBL340211 AZAPERONE 2.0 2 7.12
CHEMBL4462108 2 7.08
CHEMBL4573441 2 7.07
CHEMBL4558031 2 6.90
CHEMBL4793296 2 6.85
CHEMBL3289648 2 6.81
CHEMBL1946124 2 6.23
CHEMBL4474014 2 6.11
CHEMBL4746695 1 6.08
CHEMBL4789472 2 6.00
CHEMBL4783987 2 5.70
CHEMBL4570411 2 5.64
CHEMBL4533305 2 5.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1112 ARIPIPRAZOLE Ki = 9.7 nM 8.01
CHEMBL4574793 Ki = 26.3 nM 7.58
CHEMBL4574793 Ki = 26.0 nM 7.58
CHEMBL4753809 Ki = 54.0 nM 7.27
CHEMBL4753809 Ki = 53.7 nM 7.27
CHEMBL4743284 Ki = 58.0 nM 7.24
CHEMBL4743284 Ki = 63.1 nM 7.20
CHEMBL340211 AZAPERONE Ki = 75.86 nM 7.12
CHEMBL4462108 Ki = 83.18 nM 7.08
CHEMBL4462108 Ki = 83.0 nM 7.08
CHEMBL4573441 Ki = 86.0 nM 7.07
CHEMBL4573441 Ki = 87.1 nM 7.06
CHEMBL340211 AZAPERONE Ki = 89.7 nM 7.05
CHEMBL4558031 Ki = 125.0 nM 6.90
CHEMBL4558031 Ki = 125.89 nM 6.90
CHEMBL4793296 Ki = 141.25 nM 6.85
CHEMBL4793296 Ki = 140.0 nM 6.85
CHEMBL3289648 Ki = 156.0 nM 6.81
CHEMBL3289648 Ki = 158.49 nM 6.80
CHEMBL1946124 Ki = 588.84 nM 6.23
CHEMBL1946124 Ki = 590.0 nM 6.23
CHEMBL4474014 Ki = 774.0 nM 6.11
CHEMBL4474014 Ki = 794.33 nM 6.10
CHEMBL4746695 Ki = 840.3 nM 6.08
CHEMBL4789472 Ki = 1009.0 nM 6.00
CHEMBL4789472 Ki = 1000.0 nM 6.00
CHEMBL4783987 Ki = 1995.26 nM 5.70
CHEMBL4783987 Ki = 2089.0 nM 5.68
CHEMBL4570411 Ki = 2287.0 nM 5.64
CHEMBL4570411 Ki = 2511.89 nM 5.60
CHEMBL4533305 Ki = 3447.0 nM 5.46
CHEMBL4533305 Ki = 3467.37 nM 5.46