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Assay Detail

CHEMBL2184355

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

Binding
Displacement of [3H]ketanserin from human 5HT2AR expressed in CHOK1 cells
23
Total Activities
23
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

Discovery and pharmacological profile of new 1H-indazole-3-carboxamide and 2H-pyrrolo[3,4-c]quinoline derivatives as selective serotonin 4 receptor ligands.
Furlotti G, Alisi MA, Apicella C, Capezzone de Joannon A, Cazzolla N, Costi R, Cuzzucoli Crucitti G, Garrone B, Iacovo A, Magarò G, Mangano G, Miele G, Ombrato R, Pescatori L, Polenzani L, Rosi F, Vitiello M, Di Santo R.
J Med Chem (2012) 55 : 9446 -9466
PubMed 23043420 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 6.99 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1065 METHYSERGIDE 4.0 1 8.80
CHEMBL2179704 1 8.00
CHEMBL2179672 1 7.50
CHEMBL2177130 1 7.50
CHEMBL3216126 1 7.10
CHEMBL2179678 1 7.10
CHEMBL2179677 1 7.00
CHEMBL2179697 1 7.00
CHEMBL2179671 1 6.70
CHEMBL2179675 1 6.60
CHEMBL2179673 1 6.10
CHEMBL2179705 1 6.00
CHEMBL2179670 1 5.50
CHEMBL2179679 1 -
CHEMBL2179707 1 -
CHEMBL2179674 1 -
CHEMBL2179702 1 -
CHEMBL2179701 1 -
CHEMBL3215681 1 -
CHEMBL2179699 1 -
CHEMBL2179698 1 -
CHEMBL2179696 1 -
CHEMBL2179676 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1065 METHYSERGIDE Ki = 1.585 nM 8.80
CHEMBL2179704 Ki = 10.0 nM 8.00
CHEMBL2179672 Ki = 31.62 nM 7.50
CHEMBL2177130 Ki = 31.62 nM 7.50
CHEMBL3216126 Ki = 79.43 nM 7.10
CHEMBL2179678 Ki = 79.43 nM 7.10
CHEMBL2179677 Ki = 100.0 nM 7.00
CHEMBL2179697 Ki = 100.0 nM 7.00
CHEMBL2179671 Ki = 199.53 nM 6.70
CHEMBL2179675 Ki = 251.19 nM 6.60
CHEMBL2179673 Ki = 794.33 nM 6.10
CHEMBL2179705 Ki = 1000.0 nM 6.00
CHEMBL2179670 Ki = 3162.28 nM 5.50
CHEMBL2179679 Ki > 1000.0 nM -
CHEMBL2179707 Ki > 10000.0 nM -
CHEMBL2179674 Ki > 10000.0 nM -
CHEMBL2179702 Ki > 1000.0 nM -
CHEMBL2179701 Ki > 1000.0 nM -
CHEMBL3215681 Ki > 1000.0 nM -
CHEMBL2179699 Ki > 1000.0 nM -
CHEMBL2179698 Ki > 1000.0 nM -
CHEMBL2179696 Ki > 1000.0 nM -
CHEMBL2179676 Ki > 10000.0 nM -