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Assay Detail

CHEMBL3820049

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

Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D3 receptor incubated for 1.5 hrs by microbeta scintillation counting method
ChEMBL ↗
31
Total Activities
16
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

Development of CNS multi-receptor ligands: Modification of known D2 pharmacophores.
Etukala JR, Zhu XY, Eyunni SV, Onyameh EK, Ofori E, Bricker BA, Kang HJ, Huang XP, Roth BL, Ablordeppey SY.
Bioorg Med Chem (2016) 24 : 3671 -3679
PubMed 27364609 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 31 7.22 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3819434 — — 2 7.89
CHEMBL3818881 — — 2 7.80
CHEMBL2037526 — — 2 7.75
CHEMBL3818935 — — 2 7.68
CHEMBL3819642 — — 2 7.55
CHEMBL3818478 — — 2 7.51
CHEMBL3818799 — — 2 7.50
CHEMBL3819567 — — 2 7.50
CHEMBL3818805 — — 2 7.30
CHEMBL2037520 — — 2 7.20
CHEMBL3819153 — — 2 6.96
CHEMBL3818398 — — 2 6.79
CHEMBL3819403 — — 2 6.63
CHEMBL2037432 — — 2 6.54
CHEMBL3818124 — — 2 6.30
CHEMBL3818940 — — 1 6.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3819434 — Ki = 13.0 nM 7.89
CHEMBL3819434 — Ki = 12.88 nM 7.89
CHEMBL3818881 — Ki = 16.0 nM 7.80
CHEMBL3818881 — Ki = 16.22 nM 7.79
CHEMBL2037526 — Ki = 18.0 nM 7.75
CHEMBL2037526 — Ki = 17.78 nM 7.75
CHEMBL3818935 — Ki = 21.0 nM 7.68
CHEMBL3818935 — Ki = 20.89 nM 7.68
CHEMBL3819642 — Ki = 28.18 nM 7.55
CHEMBL3819642 — Ki = 28.0 nM 7.55
CHEMBL3818478 — Ki = 31.0 nM 7.51
CHEMBL3818799 — Ki = 31.62 nM 7.50
CHEMBL3818478 — Ki = 31.62 nM 7.50
CHEMBL3819567 — Ki = 32.0 nM 7.50
CHEMBL3819567 — Ki = 32.36 nM 7.49
CHEMBL3818799 — Ki = 33.0 nM 7.48
CHEMBL3818805 — Ki = 50.12 nM 7.30
CHEMBL3818805 — Ki = 53.0 nM 7.28
CHEMBL2037520 — Ki = 63.1 nM 7.20
CHEMBL2037520 — Ki = 64.0 nM 7.19
CHEMBL3819153 — Ki = 109.65 nM 6.96
CHEMBL3819153 — Ki = 109.0 nM 6.96
CHEMBL3818398 — Ki = 163.0 nM 6.79
CHEMBL3818398 — Ki = 162.18 nM 6.79
CHEMBL3819403 — Ki = 233.0 nM 6.63
CHEMBL3819403 — Ki = 251.19 nM 6.60
CHEMBL2037432 — Ki = 291.0 nM 6.54
CHEMBL2037432 — Ki = 288.4 nM 6.54
CHEMBL3818124 — Ki = 501.19 nM 6.30
CHEMBL3818124 — Ki = 499.0 nM 6.30
CHEMBL3818940 — Ki = 942.0 nM 6.03