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Assay Detail

CHEMBL4013335

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Functional
Agonist activity at recombinant human 5-HT2C receptor expressed in HEK293E cells assessed as induction of intracellular Ca2+ levels after 90 secs by Fluo-4-dye based FLIPR assay
ChEMBL ↗
70
Total Activities
70
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 2C (CHEMBL225) ↗
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 6.89 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4100216 — — 1 8.70
CHEMBL4081247 — — 1 8.30
CHEMBL4075267 — — 1 8.22
CHEMBL4081863 — — 1 8.22
CHEMBL4073363 — — 1 8.15
CHEMBL4085497 — — 1 7.92
CHEMBL4090637 — — 1 7.92
CHEMBL4083752 — — 1 7.89
CHEMBL4071321 — — 1 7.89
CHEMBL4091448 — — 1 7.85
CHEMBL478 CHLOROPHENYLPIPERAZINE 2.0 1 7.82
CHEMBL4082753 — — 1 7.82
CHEMBL4095663 — — 1 7.80
CHEMBL4068476 — — 1 7.77
CHEMBL4067417 — — 1 7.75
CHEMBL4100812 — — 1 7.70
CHEMBL4072217 — — 1 7.62
CHEMBL4100745 — — 1 7.60
CHEMBL4093978 — — 1 7.57
CHEMBL4083671 — — 1 7.52
CHEMBL4062681 — — 1 7.42
CHEMBL4072337 — — 1 7.39
CHEMBL4064423 — — 1 7.37
CHEMBL4082829 — — 1 7.33
CHEMBL4095818 — — 1 7.33
CHEMBL4066433 — — 1 7.24
CHEMBL4099179 — — 1 7.23
CHEMBL4093250 — — 1 7.20
CHEMBL4098357 — — 1 7.17
CHEMBL4096374 — — 1 7.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4100216 — EC50 = 2.0 nM 8.70
CHEMBL4081247 — EC50 = 5.0 nM 8.30
CHEMBL4081863 — EC50 = 6.0 nM 8.22
CHEMBL4075267 — EC50 = 6.0 nM 8.22
CHEMBL4073363 — EC50 = 7.0 nM 8.15
CHEMBL4085497 — EC50 = 12.0 nM 7.92
CHEMBL4090637 — EC50 = 12.0 nM 7.92
CHEMBL4083752 — EC50 = 13.0 nM 7.89
CHEMBL4071321 — EC50 = 13.0 nM 7.89
CHEMBL4091448 — EC50 = 14.0 nM 7.85
CHEMBL478 CHLOROPHENYLPIPERAZINE EC50 = 15.0 nM 7.82
CHEMBL4082753 — EC50 = 15.0 nM 7.82
CHEMBL4095663 — EC50 = 16.0 nM 7.80
CHEMBL4068476 — EC50 = 17.0 nM 7.77
CHEMBL4067417 — EC50 = 18.0 nM 7.75
CHEMBL4100812 — EC50 = 20.0 nM 7.70
CHEMBL4072217 — EC50 = 24.0 nM 7.62
CHEMBL4100745 — EC50 = 25.0 nM 7.60
CHEMBL4093978 — EC50 = 27.0 nM 7.57
CHEMBL4083671 — EC50 = 30.0 nM 7.52
CHEMBL4062681 — EC50 = 38.0 nM 7.42
CHEMBL4072337 — EC50 = 41.0 nM 7.39
CHEMBL4064423 — EC50 = 43.0 nM 7.37
CHEMBL4082829 — EC50 = 47.0 nM 7.33
CHEMBL4095818 — EC50 = 47.0 nM 7.33
CHEMBL4066433 — EC50 = 58.0 nM 7.24
CHEMBL4099179 — EC50 = 59.0 nM 7.23
CHEMBL4093250 — EC50 = 63.0 nM 7.20
CHEMBL4098357 — EC50 = 68.0 nM 7.17
CHEMBL4096374 — EC50 = 95.0 nM 7.02
CHEMBL4065444 — EC50 = 119.0 nM 6.92
CHEMBL4083432 — EC50 = 129.0 nM 6.89
CHEMBL4096385 — EC50 = 190.0 nM 6.72
CHEMBL4092473 — EC50 = 291.0 nM 6.54
CHEMBL4084723 — EC50 = 315.0 nM 6.50
CHEMBL4102342 — EC50 = 320.0 nM 6.50
CHEMBL4096587 — EC50 = 334.0 nM 6.48
CHEMBL4103426 — EC50 = 369.0 nM 6.43
CHEMBL4065606 — EC50 = 381.0 nM 6.42
CHEMBL4078339 — EC50 = 450.0 nM 6.35
CHEMBL4089670 — EC50 = 501.0 nM 6.30
CHEMBL4064770 — EC50 = 530.0 nM 6.28
CHEMBL4104126 — EC50 = 576.0 nM 6.24
CHEMBL4084377 — EC50 = 679.0 nM 6.17
CHEMBL4078330 — EC50 = 729.0 nM 6.14
CHEMBL4070122 — EC50 = 766.0 nM 6.12
CHEMBL4093102 — EC50 = 1032.0 nM 5.99
CHEMBL4059943 — EC50 = 1040.0 nM 5.98
CHEMBL4062613 — EC50 = 1272.0 nM 5.90
CHEMBL4088662 — EC50 = 1520.0 nM 5.82