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Assay Detail

CHEMBL617883

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

Functional
Functional activity against human 5-hydroxytryptamine 2C receptor expressed in CHO cells using fluorometric imaging plate reader
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
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
EC50 14 7.65 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL39 SEROTONIN 3.0 1 8.77
CHEMBL77880 1 8.35
CHEMBL76474 1 8.17
CHEMBL76781 1 7.75
CHEMBL80731 1 7.68
CHEMBL451543 1 7.58
CHEMBL478 CHLOROPHENYLPIPERAZINE 2.0 1 7.58
CHEMBL80482 1 7.55
CHEMBL80366 1 7.51
CHEMBL80862 1 7.40
CHEMBL76307 1 7.36
CHEMBL309760 1 7.36
CHEMBL76301 1 7.19
CHEMBL80246 1 6.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL39 SEROTONIN EC50 = 1.7 nM 8.77
CHEMBL77880 EC50 = 4.5 nM 8.35
CHEMBL76474 EC50 = 6.7 nM 8.17
CHEMBL76781 EC50 = 18.0 nM 7.75
CHEMBL80731 EC50 = 21.0 nM 7.68
CHEMBL451543 EC50 = 26.0 nM 7.58
CHEMBL478 CHLOROPHENYLPIPERAZINE EC50 = 26.0 nM 7.58
CHEMBL80482 EC50 = 28.0 nM 7.55
CHEMBL80366 EC50 = 31.0 nM 7.51
CHEMBL80862 EC50 = 40.0 nM 7.40
CHEMBL76307 EC50 = 44.0 nM 7.36
CHEMBL309760 EC50 = 44.0 nM 7.36
CHEMBL76301 EC50 = 64.0 nM 7.19
CHEMBL80246 EC50 = 130.0 nM 6.89