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Assay Detail

CHEMBL4013333

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

ADMET
Agonist activity at recombinant human 5-HT2A receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assay
70
Total Activities
70
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 2A (CHEMBL224)
Type SINGLE PROTEIN
Organism Homo sapiens

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 70 6.63 7.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4075267 1 7.12
CHEMBL4066433 1 7.03
CHEMBL4100216 1 6.82
CHEMBL478 CHLOROPHENYLPIPERAZINE 2.0 1 6.54
CHEMBL4081247 1 6.20
CHEMBL4082753 1 6.05
CHEMBL4069354 1 -
CHEMBL4064770 1 -
CHEMBL4100812 1 -
CHEMBL4093978 1 -
CHEMBL4070587 1 -
CHEMBL4081550 1 -
CHEMBL4096385 1 -
CHEMBL4078339 1 -
CHEMBL4104126 1 -
CHEMBL4086216 1 -
CHEMBL4100745 1 -
CHEMBL4092473 1 -
CHEMBL4096587 1 -
CHEMBL4095663 1 -
CHEMBL4087951 1 -
CHEMBL4066653 1 -
CHEMBL4065606 1 -
CHEMBL4093250 1 -
CHEMBL4103426 1 -
CHEMBL4085497 1 -
CHEMBL4072337 1 -
CHEMBL4093102 1 -
CHEMBL4082829 1 -
CHEMBL4090637 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4075267 EC50 = 75.0 nM 7.12
CHEMBL4066433 EC50 = 93.0 nM 7.03
CHEMBL4100216 EC50 = 151.0 nM 6.82
CHEMBL478 CHLOROPHENYLPIPERAZINE EC50 = 290.0 nM 6.54
CHEMBL4081247 EC50 = 635.0 nM 6.20
CHEMBL4082753 EC50 = 884.0 nM 6.05
CHEMBL4067417 EC50 > 10000.0 nM -
CHEMBL4092473 EC50 > 10000.0 nM -
CHEMBL4096374 EC50 > 10000.0 nM -
CHEMBL4059884 EC50 > 10000.0 nM -
CHEMBL4073363 EC50 > 10000.0 nM -
CHEMBL4083752 EC50 > 10000.0 nM -
CHEMBL4062011 EC50 > 5000.0 nM -
CHEMBL4102653 EC50 > 10000.0 nM -
CHEMBL4084723 EC50 > 10000.0 nM -
CHEMBL4064770 EC50 > 10000.0 nM -
CHEMBL4084377 EC50 > 10000.0 nM -
CHEMBL4088662 EC50 > 10000.0 nM -
CHEMBL4105011 EC50 > 10000.0 nM -
CHEMBL4080787 EC50 > 10000.0 nM -
CHEMBL4070122 EC50 > 10000.0 nM -
CHEMBL4097390 EC50 > 10000.0 nM -
CHEMBL4089670 EC50 > 10000.0 nM -
CHEMBL4078330 EC50 > 10000.0 nM -
CHEMBL4062613 EC50 > 10000.0 nM -
CHEMBL4090579 EC50 > 10000.0 nM -
CHEMBL4061625 EC50 > 10000.0 nM -
CHEMBL4083432 EC50 > 10000.0 nM -
CHEMBL4095663 EC50 > 10000.0 nM -
CHEMBL4090637 EC50 > 10000.0 nM -
CHEMBL4082829 EC50 > 10000.0 nM -
CHEMBL4093102 EC50 > 10000.0 nM -
CHEMBL4072337 EC50 > 10000.0 nM -
CHEMBL4085497 EC50 > 10000.0 nM -
CHEMBL4103426 EC50 > 10000.0 nM -
CHEMBL4093250 EC50 > 10000.0 nM -
CHEMBL4065606 EC50 > 10000.0 nM -
CHEMBL4066653 EC50 > 10000.0 nM -
CHEMBL4087951 EC50 > 10000.0 nM -
CHEMBL4100745 EC50 > 5000.0 nM -
CHEMBL4096587 EC50 > 10000.0 nM -
CHEMBL4069354 EC50 > 10000.0 nM -
CHEMBL4100812 EC50 > 5000.0 nM -
CHEMBL4093978 EC50 > 10000.0 nM -
CHEMBL4070587 EC50 > 10000.0 nM -
CHEMBL4081550 EC50 > 10000.0 nM -
CHEMBL4096385 EC50 > 10000.0 nM -
CHEMBL4078339 EC50 >= 1800.0 nM -
CHEMBL4104126 EC50 > 5000.0 nM -
CHEMBL4086216 EC50 > 5000.0 nM -