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Assay Detail

CHEMBL3820050

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

Binding
Displacement of [3H]N-methylspiperone from human recombinant dopamine D4 receptor incubated for 1.5 hrs by microbeta scintillation counting method
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(4) dopamine receptor (CHEMBL219)
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 6.69 8.81

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3818478 2 8.81
CHEMBL3818805 2 7.80
CHEMBL3818799 2 7.17
CHEMBL3818935 2 6.93
CHEMBL3819567 2 6.88
CHEMBL2037432 2 6.85
CHEMBL2037526 2 6.79
CHEMBL3819642 2 6.79
CHEMBL3818940 1 6.64
CHEMBL3819434 2 6.37
CHEMBL3818881 2 6.29
CHEMBL3818398 2 6.17
CHEMBL3819153 2 6.08
CHEMBL3819403 2 5.92
CHEMBL3818124 2 5.82
CHEMBL2037520 2 5.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3818478 Ki = 1.549 nM 8.81
CHEMBL3818478 Ki = 1.6 nM 8.80
CHEMBL3818805 Ki = 16.0 nM 7.80
CHEMBL3818805 Ki = 16.22 nM 7.79
CHEMBL3818799 Ki = 67.61 nM 7.17
CHEMBL3818799 Ki = 68.0 nM 7.17
CHEMBL3818935 Ki = 118.0 nM 6.93
CHEMBL3818935 Ki = 117.49 nM 6.93
CHEMBL3819567 Ki = 132.0 nM 6.88
CHEMBL3819567 Ki = 131.83 nM 6.88
CHEMBL2037432 Ki = 141.25 nM 6.85
CHEMBL2037432 Ki = 140.0 nM 6.85
CHEMBL2037526 Ki = 162.18 nM 6.79
CHEMBL2037526 Ki = 162.0 nM 6.79
CHEMBL3819642 Ki = 162.18 nM 6.79
CHEMBL3819642 Ki = 163.0 nM 6.79
CHEMBL3818940 Ki = 229.0 nM 6.64
CHEMBL3819434 Ki = 432.0 nM 6.37
CHEMBL3819434 Ki = 436.52 nM 6.36
CHEMBL3818881 Ki = 508.0 nM 6.29
CHEMBL3818881 Ki = 512.86 nM 6.29
CHEMBL3818398 Ki = 671.0 nM 6.17
CHEMBL3818398 Ki = 676.08 nM 6.17
CHEMBL3819153 Ki = 831.76 nM 6.08
CHEMBL3819153 Ki = 841.0 nM 6.08
CHEMBL3819403 Ki = 1217.0 nM 5.92
CHEMBL3819403 Ki = 1230.27 nM 5.91
CHEMBL3818124 Ki = 1512.0 nM 5.82
CHEMBL3818124 Ki = 1584.89 nM 5.80
CHEMBL2037520 Ki = 1698.24 nM 5.77
CHEMBL2037520 Ki = 1710.0 nM 5.77