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Assay Detail

CHEMBL5046639

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

Binding
Displacement of [3H]-LSD from human 5-HT7 receptor transfected in CHO-K1 cells measured after 120 mins by scintillation counting method
22
Total Activities
22
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

5-hydroxytryptamine receptor 7 (CHEMBL3155)
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 22 7.28 9.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL93240 METITEPINE 2.0 1 9.25
CHEMBL5084167 1 7.81
CHEMBL5080955 1 7.73
CHEMBL5082182 1 7.67
CHEMBL5077755 1 7.66
CHEMBL5080305 1 7.58
CHEMBL5090557 1 7.42
CHEMBL5088232 1 7.36
CHEMBL5089348 1 7.33
CHEMBL5093250 1 7.32
CHEMBL5076846 1 7.31
CHEMBL5077178 1 7.20
CHEMBL5082267 1 7.17
CHEMBL5087742 1 7.02
CHEMBL5076882 1 6.99
CHEMBL5083505 1 6.99
CHEMBL5093017 1 6.90
CHEMBL5073337 1 6.90
CHEMBL5085390 1 6.80
CHEMBL5080719 1 6.75
CHEMBL5092755 1 6.69
CHEMBL5079536 1 6.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL93240 METITEPINE Ki = 0.5623 nM 9.25
CHEMBL5084167 Ki = 15.49 nM 7.81
CHEMBL5080955 Ki = 18.62 nM 7.73
CHEMBL5082182 Ki = 21.38 nM 7.67
CHEMBL5077755 Ki = 21.88 nM 7.66
CHEMBL5080305 Ki = 26.3 nM 7.58
CHEMBL5090557 Ki = 38.02 nM 7.42
CHEMBL5088232 Ki = 43.65 nM 7.36
CHEMBL5089348 Ki = 46.77 nM 7.33
CHEMBL5093250 Ki = 47.86 nM 7.32
CHEMBL5076846 Ki = 48.98 nM 7.31
CHEMBL5077178 Ki = 63.1 nM 7.20
CHEMBL5082267 Ki = 67.61 nM 7.17
CHEMBL5087742 Ki = 95.5 nM 7.02
CHEMBL5076882 Ki = 102.33 nM 6.99
CHEMBL5083505 Ki = 102.33 nM 6.99
CHEMBL5093017 Ki = 125.89 nM 6.90
CHEMBL5073337 Ki = 125.89 nM 6.90
CHEMBL5085390 Ki = 158.49 nM 6.80
CHEMBL5080719 Ki = 177.83 nM 6.75
CHEMBL5092755 Ki = 204.17 nM 6.69
CHEMBL5079536 Ki = 416.87 nM 6.38