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Assay Detail

CHEMBL4368222

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

Binding
Displacement of [3H]Spiperone from human D2S receptor expressed in CHOK1 cell membranes measured after 120 mins
19
Total Activities
19
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

Synthesis, pharmacological and structural studies of 5-substituted-3-(1-arylmethyl-1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles as multi-target ligands of aminergic GPCRs.
Kondej M, Wróbel TM, Silva AG, Stępnicki P, Koszła O, Kędzierska E, Bartyzel A, Biała G, Matosiuk D, Loza MI, Castro M, Kaczor AA.
Eur J Med Chem (2019) 180 : 673 -689
PubMed 31357129 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 6.98 8.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 8.49
CHEMBL285157 1 7.59
CHEMBL4552542 1 7.57
CHEMBL366081 1 7.20
CHEMBL4554558 1 7.14
CHEMBL4565126 1 7.06
CHEMBL4578143 1 6.97
CHEMBL4460564 1 6.95
CHEMBL4466356 1 6.88
CHEMBL4543263 1 6.85
CHEMBL4444351 1 6.85
CHEMBL4449936 1 6.83
CHEMBL4454000 1 6.82
CHEMBL4548632 1 6.78
CHEMBL4527257 1 6.78
CHEMBL4521477 1 6.59
CHEMBL4460839 1 6.52
CHEMBL4457881 1 6.49
CHEMBL4558444 1 6.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 3.25 nM 8.49
CHEMBL285157 Ki = 25.8 nM 7.59
CHEMBL4552542 Ki = 26.9 nM 7.57
CHEMBL366081 Ki = 62.7 nM 7.20
CHEMBL4554558 Ki = 71.9 nM 7.14
CHEMBL4565126 Ki = 87.3 nM 7.06
CHEMBL4578143 Ki = 108.0 nM 6.97
CHEMBL4460564 Ki = 112.0 nM 6.95
CHEMBL4466356 Ki = 132.0 nM 6.88
CHEMBL4543263 Ki = 142.0 nM 6.85
CHEMBL4444351 Ki = 141.0 nM 6.85
CHEMBL4449936 Ki = 148.0 nM 6.83
CHEMBL4454000 Ki = 151.0 nM 6.82
CHEMBL4548632 Ki = 165.0 nM 6.78
CHEMBL4527257 Ki = 166.0 nM 6.78
CHEMBL4521477 Ki = 257.0 nM 6.59
CHEMBL4460839 Ki = 299.0 nM 6.52
CHEMBL4457881 Ki = 321.0 nM 6.49
CHEMBL4558444 Ki = 465.0 nM 6.33