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Assay Detail

CHEMBL620618

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

Binding
Affinity for human 5-hydroxytryptamine 2C receptor expressed in mammalian cell line
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 2C (CHEMBL225)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Indoline derivatives as 5-HT(2C) receptor agonists.
Bentley JM, Adams DR, Bebbington D, Benwell KR, Bickerdike MJ, Davidson JE, Dawson CE, Dourish CT, Duncton MA, Gaur S, George AR, Giles PR, Hamlyn RJ, Kennett GA, Knight AR, Malcolm CS, Mansell HL, Misra A, Monck NJ, Pratt RM, Quirk K, Roffey JR, Vickers SP, Cliffe IA.
Bioorg Med Chem Lett (2004) 14 : 2367 -2370
PubMed 15081042 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 7.98 8.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL76781 1 8.64
CHEMBL76474 1 8.49
CHEMBL451543 1 8.24
CHEMBL80731 1 8.19
CHEMBL39 SEROTONIN 3.0 1 8.16
CHEMBL77880 1 8.06
CHEMBL478 CHLOROPHENYLPIPERAZINE 2.0 1 8.05
CHEMBL76307 1 7.89
CHEMBL80366 1 7.85
CHEMBL80862 1 7.80
CHEMBL76301 1 7.77
CHEMBL309760 1 7.62
CHEMBL80246 1 7.58
CHEMBL80482 1 7.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL76781 Ki = 2.3 nM 8.64
CHEMBL76474 Ki = 3.2 nM 8.49
CHEMBL451543 Ki = 5.7 nM 8.24
CHEMBL80731 Ki = 6.4 nM 8.19
CHEMBL39 SEROTONIN Ki = 6.9 nM 8.16
CHEMBL77880 Ki = 8.7 nM 8.06
CHEMBL478 CHLOROPHENYLPIPERAZINE Ki = 9.0 nM 8.05
CHEMBL76307 Ki = 13.0 nM 7.89
CHEMBL80366 Ki = 14.0 nM 7.85
CHEMBL80862 Ki = 16.0 nM 7.80
CHEMBL76301 Ki = 17.0 nM 7.77
CHEMBL309760 Ki = 24.0 nM 7.62
CHEMBL80246 Ki = 26.0 nM 7.58
CHEMBL80482 Ki = 38.0 nM 7.42