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Assay Detail

CHEMBL4681097

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Functional
Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay
ChEMBL ↗
88
Total Activities
44
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Flp-In-293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Design and Discovery of Functionally Selective Serotonin 2C (5-HT) Receptor Agonists.
Cheng J,McCorvy JD,Giguere PM,Zhu H,Kenakin T,Roth BL,Kozikowski AP
J Med Chem (2016) 59 : 9866 -9880
PubMed 27726356 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 71 6.50 8.63
pEC50 17 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL39 SEROTONIN 3.0 2 8.63
CHEMBL4779260 — — 2 7.66
CHEMBL4751981 — — 2 7.43
CHEMBL4756903 — — 2 6.96
CHEMBL4739937 — — 2 6.96
CHEMBL4790652 — — 2 6.95
CHEMBL4761526 — — 2 6.93
CHEMBL4790992 — — 2 6.67
CHEMBL360328 LORCASERIN 4.0 2 6.61
CHEMBL4753812 — — 2 6.59
CHEMBL4777303 — — 2 6.53
CHEMBL4759181 — — 2 6.53
CHEMBL4759878 — — 2 6.45
CHEMBL4762225 — — 2 6.41
CHEMBL4782824 — — 2 6.41
CHEMBL4757214 — — 2 6.34
CHEMBL4800666 — — 2 6.23
CHEMBL4743977 — — 2 6.21
CHEMBL4752412 — — 2 6.13
CHEMBL4758641 — — 2 6.12
CHEMBL4748110 — — 2 6.03
CHEMBL4786831 — — 2 6.03
CHEMBL4789310 — — 2 6.01
CHEMBL4757142 — — 2 5.71
CHEMBL4761064 — — 2 5.66
CHEMBL4752976 — — 2 5.63
CHEMBL4740346 — — 2 5.58
CHEMBL4762474 — — 2 -
CHEMBL4760851 — — 2 -
CHEMBL4750271 — — 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL39 SEROTONIN EC50 = 2.344 nM 8.63
CHEMBL39 SEROTONIN EC50 = 2.35 nM 8.63
CHEMBL4779260 — EC50 = 22.0 nM 7.66
CHEMBL4779260 — EC50 = 22.39 nM 7.65
CHEMBL4751981 — EC50 = 37.0 nM 7.43
CHEMBL4751981 — EC50 = 37.15 nM 7.43
CHEMBL4756903 — EC50 = 111.0 nM 6.96
CHEMBL4756903 — EC50 = 109.65 nM 6.96
CHEMBL4739937 — EC50 = 109.0 nM 6.96
CHEMBL4739937 — EC50 = 109.65 nM 6.96
CHEMBL4790652 — EC50 = 113.0 nM 6.95
CHEMBL4790652 — EC50 = 112.2 nM 6.95
CHEMBL4761526 — EC50 = 117.0 nM 6.93
CHEMBL4761526 — EC50 = 117.49 nM 6.93
CHEMBL4790992 — EC50 = 213.8 nM 6.67
CHEMBL4790992 — EC50 = 213.0 nM 6.67
CHEMBL360328 LORCASERIN EC50 = 248.0 nM 6.61
CHEMBL360328 LORCASERIN EC50 = 245.47 nM 6.61
CHEMBL4753812 — EC50 = 257.04 nM 6.59
CHEMBL4753812 — EC50 = 260.0 nM 6.58
CHEMBL4777303 — EC50 = 295.0 nM 6.53
CHEMBL4777303 — EC50 = 295.12 nM 6.53
CHEMBL4759181 — EC50 = 295.12 nM 6.53
CHEMBL4759181 — EC50 = 298.0 nM 6.53
CHEMBL4759878 — EC50 = 358.0 nM 6.45
CHEMBL4759878 — EC50 = 354.81 nM 6.45
CHEMBL4762225 — EC50 = 393.0 nM 6.41
CHEMBL4762225 — EC50 = 389.05 nM 6.41
CHEMBL4782824 — EC50 = 392.0 nM 6.41
CHEMBL4782824 — EC50 = 389.05 nM 6.41
CHEMBL4757214 — EC50 = 456.0 nM 6.34
CHEMBL4757214 — EC50 = 457.09 nM 6.34
CHEMBL4800666 — EC50 = 585.0 nM 6.23
CHEMBL4800666 — EC50 = 588.84 nM 6.23
CHEMBL4743977 — EC50 = 618.0 nM 6.21
CHEMBL4743977 — EC50 = 630.96 nM 6.20
CHEMBL4752412 — EC50 = 741.31 nM 6.13
CHEMBL4752412 — EC50 = 749.0 nM 6.13
CHEMBL4758641 — EC50 = 754.0 nM 6.12
CHEMBL4758641 — EC50 = 758.58 nM 6.12
CHEMBL4786831 — EC50 = 938.0 nM 6.03
CHEMBL4786831 — EC50 = 933.25 nM 6.03
CHEMBL4748110 — EC50 = 933.25 nM 6.03
CHEMBL4748110 — EC50 = 939.0 nM 6.03
CHEMBL4789310 — EC50 = 977.24 nM 6.01
CHEMBL4789310 — EC50 = 976.0 nM 6.01
CHEMBL4757142 — EC50 = 1960.0 nM 5.71
CHEMBL4757142 — EC50 = 1949.84 nM 5.71
CHEMBL4761064 — EC50 = 2210.0 nM 5.66
CHEMBL4761064 — EC50 = 2187.76 nM 5.66