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Assay Detail

CHEMBL5046637

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

Binding
Displacement of [3H]-ketanserin from human human 5-HT2A receptor transfected in CHO-K1 cells measured after 60 mins by scintillation counting method
26
Total Activities
26
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 2A (CHEMBL224)
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 26 8.37 9.61

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5084167 1 9.61
CHEMBL5076846 1 9.19
CHEMBL5090557 1 9.16
CHEMBL5088232 1 8.82
CHEMBL5092755 1 8.77
CHEMBL5077755 1 8.77
CHEMBL715 OLANZAPINE 4.0 1 8.72
CHEMBL5089348 1 8.71
CHEMBL93240 METITEPINE 2.0 1 8.70
CHEMBL5080719 1 8.56
CHEMBL5082267 1 8.53
CHEMBL5093017 1 8.45
CHEMBL5076882 1 8.41
CHEMBL5087742 1 8.38
CHEMBL5073337 1 8.38
CHEMBL5082182 1 8.36
CHEMBL5080305 1 8.23
CHEMBL5080955 1 8.20
CHEMBL5079536 1 8.16
CHEMBL71 CHLORPROMAZINE 4.0 1 7.92
CHEMBL5085390 1 7.89
CHEMBL5093250 1 7.89
CHEMBL5077178 1 7.87
CHEMBL54 HALOPERIDOL 4.0 1 7.64
CHEMBL5083505 1 7.40
CHEMBL716 QUETIAPINE 4.0 1 6.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5084167 Ki = 0.2455 nM 9.61
CHEMBL5076846 Ki = 0.6457 nM 9.19
CHEMBL5090557 Ki = 0.6918 nM 9.16
CHEMBL5088232 Ki = 1.514 nM 8.82
CHEMBL5092755 Ki = 1.698 nM 8.77
CHEMBL5077755 Ki = 1.698 nM 8.77
CHEMBL715 OLANZAPINE Ki = 1.905 nM 8.72
CHEMBL5089348 Ki = 1.95 nM 8.71
CHEMBL93240 METITEPINE Ki = 1.995 nM 8.70
CHEMBL5080719 Ki = 2.754 nM 8.56
CHEMBL5082267 Ki = 2.951 nM 8.53
CHEMBL5093017 Ki = 3.548 nM 8.45
CHEMBL5076882 Ki = 3.89 nM 8.41
CHEMBL5087742 Ki = 4.169 nM 8.38
CHEMBL5073337 Ki = 4.169 nM 8.38
CHEMBL5082182 Ki = 4.365 nM 8.36
CHEMBL5080305 Ki = 5.888 nM 8.23
CHEMBL5080955 Ki = 6.31 nM 8.20
CHEMBL5079536 Ki = 6.918 nM 8.16
CHEMBL71 CHLORPROMAZINE Ki = 12.02 nM 7.92
CHEMBL5085390 Ki = 12.88 nM 7.89
CHEMBL5093250 Ki = 12.88 nM 7.89
CHEMBL5077178 Ki = 13.49 nM 7.87
CHEMBL54 HALOPERIDOL Ki = 22.91 nM 7.64
CHEMBL5083505 Ki = 39.81 nM 7.40
CHEMBL716 QUETIAPINE Ki = 120.23 nM 6.92