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Assay Detail

CHEMBL4013369

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

Binding
Agonist activity at recombinant human 5-HT2C receptor D134A mutant expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Utilization of an Active Site Mutant Receptor for the Identification of Potent and Selective Atypical 5-HT2C Receptor Agonists.
Carpenter J, Wang Y, Wu G, Feng J, Ye XY, Morales CL, Broekema M, Rossi KA, Miller KJ, Murphy BJ, Wu G, Malmstrom SE, Azzara AV, Sher PM, Fevig JM, Alt A, Bertekap RL, Cullen MJ, Harper TM, Foster K, Luk E, Xiang Q, Grubb MF, Robl JA, Wacker DA.
J Med Chem (2017) 60 : 6166 -6190
PubMed 28635286 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 7.80 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4065444 1 8.70
CHEMBL4064423 1 6.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4065444 EC50 = 2.0 nM 8.70
CHEMBL4064423 EC50 = 130.0 nM 6.89