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Assay Detail

CHEMBL926600

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Functional
Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation
ChEMBL ↗
37
Total Activities
37
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 Intermediate

Target

5-hydroxytryptamine receptor 2B (CHEMBL1833) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and structure-activity relationship of (1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-benzazepine (Lorcaserin), a selective serotonin 5-HT2C receptor agonist for the treatment of obesity.
Smith BM, Smith JM, Tsai JH, Schultz JA, Gilson CA, Estrada SA, Chen RR, Park DM, Prieto EB, Gallardo CS, Sengupta D, Dosa PI, Covel JA, Ren A, Webb RR, Beeley NR, Martin M, Morgan M, Espitia S, Saldana HR, Bjenning C, Whelan KT, Grottick AJ, Menzaghi F, Thomsen WJ.
J Med Chem (2008) 51 : 305 -313
PubMed 18095642 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 37 6.50 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL76781 — — 1 8.80
CHEMBL253811 NORDEXFENFLURAMINE — 1 7.80
CHEMBL39 SEROTONIN 3.0 1 7.60
CHEMBL400600 — — 1 7.40
CHEMBL478 CHLOROPHENYLPIPERAZINE 2.0 1 7.40
CHEMBL253591 — — 1 7.40
CHEMBL178366 — — 1 7.30
CHEMBL181787 — — 1 7.20
CHEMBL399750 — — 1 6.70
CHEMBL253805 — — 1 6.60
CHEMBL253809 — — 1 6.60
CHEMBL360492 — — 1 6.50
CHEMBL253806 — — 1 6.40
CHEMBL254009 — — 1 6.30
CHEMBL181672 — — 1 6.30
CHEMBL253810 — — 1 6.20
CHEMBL179337 — — 1 6.10
CHEMBL254215 — — 1 6.10
CHEMBL178124 — — 1 6.10
CHEMBL360328 LORCASERIN 4.0 1 6.10
CHEMBL180668 — — 1 6.00
CHEMBL181172 — — 1 6.00
CHEMBL181076 — — 1 5.90
CHEMBL178365 — — 1 5.90
CHEMBL178231 — — 1 5.80
CHEMBL440752 — — 1 5.70
CHEMBL368016 — — 1 5.60
CHEMBL367796 — — 1 5.40
CHEMBL361742 — — 1 5.30
CHEMBL253155 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL76781 — EC50 = 1.585 nM 8.80
CHEMBL253811 NORDEXFENFLURAMINE EC50 = 15.85 nM 7.80
CHEMBL39 SEROTONIN EC50 = 25.12 nM 7.60
CHEMBL400600 — EC50 = 39.81 nM 7.40
CHEMBL478 CHLOROPHENYLPIPERAZINE EC50 = 39.81 nM 7.40
CHEMBL253591 — EC50 = 39.81 nM 7.40
CHEMBL178366 — EC50 = 50.12 nM 7.30
CHEMBL181787 — EC50 = 63.1 nM 7.20
CHEMBL399750 — EC50 = 199.53 nM 6.70
CHEMBL253805 — EC50 = 251.19 nM 6.60
CHEMBL253809 — EC50 = 251.19 nM 6.60
CHEMBL360492 — EC50 = 316.23 nM 6.50
CHEMBL253806 — EC50 = 398.11 nM 6.40
CHEMBL254009 — EC50 = 501.19 nM 6.30
CHEMBL181672 — EC50 = 501.19 nM 6.30
CHEMBL253810 — EC50 = 630.96 nM 6.20
CHEMBL360328 LORCASERIN EC50 = 794.33 nM 6.10
CHEMBL178124 — EC50 = 794.33 nM 6.10
CHEMBL179337 — EC50 = 794.33 nM 6.10
CHEMBL254215 — EC50 = 794.33 nM 6.10
CHEMBL180668 — EC50 = 1000.0 nM 6.00
CHEMBL181172 — EC50 = 1000.0 nM 6.00
CHEMBL181076 — EC50 = 1258.93 nM 5.90
CHEMBL178365 — EC50 = 1258.93 nM 5.90
CHEMBL178231 — EC50 = 1584.89 nM 5.80
CHEMBL440752 — EC50 = 1995.26 nM 5.70
CHEMBL368016 — EC50 = 2511.89 nM 5.60
CHEMBL367796 — EC50 = 3981.07 nM 5.40
CHEMBL361742 — EC50 = 5011.87 nM 5.30
CHEMBL253155 — EC50 < 10000.0 nM -
CHEMBL181324 — EC50 < 10000.0 nM -
CHEMBL178252 — EC50 < 10000.0 nM -
CHEMBL360479 — EC50 < 10000.0 nM -
CHEMBL362073 — EC50 < 10000.0 nM -
CHEMBL178566 — EC50 < 10000.0 nM -
CHEMBL253807 — EC50 < 10000.0 nM -
CHEMBL398926 — EC50 < 10000.0 nM -