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Assay Detail

CHEMBL5046640

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

Binding
Displacement of [3H]-methylspiperone from human D2 receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

D(2) dopamine receptor (CHEMBL217)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Multifunctional Arylsulfone and Arylsulfonamide-Based Ligands with Prominent Mood-Modulating Activity and Benign Safety Profile, Targeting Neuropsychiatric Symptoms of Dementia.
Marcinkowska M, Bucki A, Sniecikowska J, Zagórska A, Fajkis-Zajączkowska N, Siwek A, Gluch-Lutwin M, Żmudzki P, Jastrzebska-Wiesek M, Partyka A, Wesołowska A, Abram M, Przejczowska-Pomierny K, Cios A, Wyska E, Mika K, Kotańska M, Mierzejewski P, Kolaczkowski M.
J Med Chem (2021) 64 : 12603 -12629
PubMed 34436892 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 7.19 8.73

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 8.73
CHEMBL71 CHLORPROMAZINE 4.0 1 8.63
CHEMBL5084167 1 8.28
CHEMBL715 OLANZAPINE 4.0 1 7.77
CHEMBL5092755 1 7.70
CHEMBL5080719 1 7.52
CHEMBL5088232 1 7.33
CHEMBL5077755 1 7.30
CHEMBL5079536 1 7.27
CHEMBL5076846 1 7.27
CHEMBL5087742 1 7.27
CHEMBL5090557 1 7.26
CHEMBL5080305 1 7.03
CHEMBL5089348 1 7.02
CHEMBL5073337 1 6.95
CHEMBL5093017 1 6.89
CHEMBL5080955 1 6.87
CHEMBL5076882 1 6.81
CHEMBL5085390 1 6.81
CHEMBL5082182 1 6.79
CHEMBL5077178 1 6.59
CHEMBL5082267 1 6.52
CHEMBL716 QUETIAPINE 4.0 1 6.51
CHEMBL5093250 1 6.37
CHEMBL5083505 1 6.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 1.862 nM 8.73
CHEMBL71 CHLORPROMAZINE Ki = 2.344 nM 8.63
CHEMBL5084167 Ki = 5.248 nM 8.28
CHEMBL715 OLANZAPINE Ki = 16.98 nM 7.77
CHEMBL5092755 Ki = 19.95 nM 7.70
CHEMBL5080719 Ki = 30.2 nM 7.52
CHEMBL5088232 Ki = 46.77 nM 7.33
CHEMBL5077755 Ki = 50.12 nM 7.30
CHEMBL5079536 Ki = 53.7 nM 7.27
CHEMBL5076846 Ki = 53.7 nM 7.27
CHEMBL5087742 Ki = 53.7 nM 7.27
CHEMBL5090557 Ki = 54.95 nM 7.26
CHEMBL5080305 Ki = 93.33 nM 7.03
CHEMBL5089348 Ki = 95.5 nM 7.02
CHEMBL5073337 Ki = 112.2 nM 6.95
CHEMBL5093017 Ki = 128.82 nM 6.89
CHEMBL5080955 Ki = 134.9 nM 6.87
CHEMBL5076882 Ki = 154.88 nM 6.81
CHEMBL5085390 Ki = 154.88 nM 6.81
CHEMBL5082182 Ki = 162.18 nM 6.79
CHEMBL5077178 Ki = 257.04 nM 6.59
CHEMBL5082267 Ki = 302.0 nM 6.52
CHEMBL716 QUETIAPINE Ki = 309.03 nM 6.51
CHEMBL5093250 Ki = 426.58 nM 6.37
CHEMBL5083505 Ki = 645.65 nM 6.19