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Assay Detail

CHEMBL918970

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Functional
Activity at human 5HT2C expressed in HEK293E cells assessed as elevation of intracellular calcium by 384-FLIPR assay
ChEMBL ↗
48
Total Activities
48
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293E
Confidence 9 — Direct single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 2C (CHEMBL225) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of (R)-9-ethyl-1,3,4,10b-tetrahydro-7-trifluoromethylpyrazino[2,1-a]isoindol- 6(2H)-one, a selective, orally active agonist of the 5-HT(2C) receptor.
Wacker DA, Varnes JG, Malmstrom SE, Cao X, Hung CP, Ung T, Wu G, Zhang G, Zuvich E, Thomas MA, Keim WJ, Cullen MJ, Rohrbach KW, Qu Q, Narayanan R, Rossi K, Janovitz E, Lehman-McKeeman L, Malley MF, Devenny J, Pelleymounter MA, Miller KJ, Robl JA.
J Med Chem (2007) 50 : 1365 -1379
PubMed 17315987 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 48 7.22 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL223468 — — 1 8.85
CHEMBL373531 — — 1 8.30
CHEMBL374562 — — 1 8.22
CHEMBL222514 — — 1 8.15
CHEMBL2113264 — — 1 8.00
CHEMBL220211 — — 1 7.96
CHEMBL385577 — — 1 7.92
CHEMBL375170 — — 1 7.85
CHEMBL478 CHLOROPHENYLPIPERAZINE 2.0 1 7.82
CHEMBL221113 — — 1 7.80
CHEMBL374436 — — 1 7.77
CHEMBL223272 — — 1 7.75
CHEMBL220900 — — 1 7.70
CHEMBL220274 — — 1 7.62
CHEMBL219734 — — 1 7.58
CHEMBL219837 — — 1 7.55
CHEMBL375575 — — 1 7.46
CHEMBL223896 — — 1 7.43
CHEMBL220207 — — 1 7.38
CHEMBL222566 — — 1 7.37
CHEMBL223466 — — 1 7.34
CHEMBL223440 — — 1 7.31
CHEMBL223292 — — 1 7.27
CHEMBL220833 — — 1 7.27
CHEMBL374660 — — 1 7.20
CHEMBL373695 — — 1 7.14
CHEMBL376676 — — 1 7.09
CHEMBL220157 — — 1 7.07
CHEMBL373905 — — 1 7.03
CHEMBL223628 — — 1 6.97

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL223468 — EC50 = 1.4 nM 8.85
CHEMBL373531 — EC50 = 5.0 nM 8.30
CHEMBL374562 — EC50 = 6.0 nM 8.22
CHEMBL222514 — EC50 = 7.0 nM 8.15
CHEMBL2113264 — EC50 = 10.0 nM 8.00
CHEMBL220211 — EC50 = 11.0 nM 7.96
CHEMBL385577 — EC50 = 12.0 nM 7.92
CHEMBL375170 — EC50 = 14.0 nM 7.85
CHEMBL478 CHLOROPHENYLPIPERAZINE EC50 = 15.0 nM 7.82
CHEMBL221113 — EC50 = 16.0 nM 7.80
CHEMBL374436 — EC50 = 17.0 nM 7.77
CHEMBL223272 — EC50 = 18.0 nM 7.75
CHEMBL220900 — EC50 = 20.0 nM 7.70
CHEMBL220274 — EC50 = 24.0 nM 7.62
CHEMBL219734 — EC50 = 26.0 nM 7.58
CHEMBL219837 — EC50 = 28.0 nM 7.55
CHEMBL375575 — EC50 = 35.0 nM 7.46
CHEMBL223896 — EC50 = 37.0 nM 7.43
CHEMBL220207 — EC50 = 42.0 nM 7.38
CHEMBL222566 — EC50 = 43.0 nM 7.37
CHEMBL223466 — EC50 = 46.0 nM 7.34
CHEMBL223440 — EC50 = 49.0 nM 7.31
CHEMBL223292 — EC50 = 54.0 nM 7.27
CHEMBL220833 — EC50 = 54.0 nM 7.27
CHEMBL374660 — EC50 = 63.0 nM 7.20
CHEMBL373695 — EC50 = 72.0 nM 7.14
CHEMBL376676 — EC50 = 82.0 nM 7.09
CHEMBL220157 — EC50 = 86.0 nM 7.07
CHEMBL373905 — EC50 = 94.0 nM 7.03
CHEMBL223628 — EC50 = 107.0 nM 6.97
CHEMBL376456 — EC50 = 136.0 nM 6.87
CHEMBL222466 — EC50 = 246.0 nM 6.61
CHEMBL223090 — EC50 = 281.0 nM 6.55
CHEMBL375642 — EC50 = 296.0 nM 6.53
CHEMBL373483 — EC50 = 363.0 nM 6.44
CHEMBL375302 — EC50 = 480.0 nM 6.32
CHEMBL373402 — EC50 = 478.0 nM 6.32
CHEMBL387344 — EC50 = 514.0 nM 6.29
CHEMBL376455 — EC50 = 1500.0 nM 5.82
CHEMBL220789 — EC50 = 1580.0 nM 5.80
CHEMBL223469 — EC50 = 1730.0 nM 5.76
CHEMBL223584 — EC50 = 1840.0 nM 5.74
CHEMBL220521 — EC50 - — -
CHEMBL220115 — EC50 - — -
CHEMBL374659 — EC50 - — -
CHEMBL223441 — EC50 - — -
CHEMBL374463 — EC50 - — -
CHEMBL223271 — EC50 > 10000.0 nM -