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Assay Detail

CHEMBL987061

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Functional
Agonist activity at human thrombopoietin receptor in Ba/F3 cells assessed as activation of Stat5 response element-driven reporter gene expression
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type BaF3
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Thrombopoietin receptor (CHEMBL1864)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and biological evaluation of benzo[a]carbazole-based small molecule agonists of the thrombopoietin (Tpo) receptor.
Alper PB, Marsilje TH, Mutnick D, Lu W, Chatterjee A, Roberts MJ, He Y, Karanewsky DS, Chow D, Lao J, Gerken A, Tuntland T, Liu B, Chang J, Gordon P, Seidel HM, Tian SS.
Bioorg Med Chem Lett (2008) 18 : 5255 -5258
PubMed 18778936 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 37 6.60 7.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL479081 1 7.58
CHEMBL477381 1 7.46
CHEMBL461101 ELTROMBOPAG 4.0 1 7.42
CHEMBL518285 1 7.39
CHEMBL479083 1 7.37
CHEMBL477400 1 7.26
CHEMBL477174 1 7.19
CHEMBL477175 1 7.17
CHEMBL516272 1 7.12
CHEMBL477195 1 6.96
CHEMBL489367 1 6.96
CHEMBL477401 1 6.92
CHEMBL479093 1 6.90
CHEMBL491798 1 6.84
CHEMBL515795 1 6.83
CHEMBL521746 1 6.71
CHEMBL492017 1 6.63
CHEMBL476556 1 6.55
CHEMBL523460 1 6.48
CHEMBL489365 1 6.43
CHEMBL479082 1 6.34
CHEMBL490585 1 6.33
CHEMBL521768 1 6.25
CHEMBL490586 1 6.10
CHEMBL489388 1 6.06
CHEMBL490412 1 5.89
CHEMBL490409 1 5.47
CHEMBL523147 1 5.11
CHEMBL448025 1 5.11
CHEMBL522978 1 5.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL479081 EC50 = 26.0 nM 7.58
CHEMBL477381 EC50 = 35.0 nM 7.46
CHEMBL461101 ELTROMBOPAG EC50 = 38.0 nM 7.42
CHEMBL518285 EC50 = 41.0 nM 7.39
CHEMBL479083 EC50 = 43.0 nM 7.37
CHEMBL477400 EC50 = 55.0 nM 7.26
CHEMBL477174 EC50 = 65.0 nM 7.19
CHEMBL477175 EC50 = 67.0 nM 7.17
CHEMBL516272 EC50 = 76.0 nM 7.12
CHEMBL489367 EC50 = 109.0 nM 6.96
CHEMBL477195 EC50 = 111.0 nM 6.96
CHEMBL477401 EC50 = 119.0 nM 6.92
CHEMBL479093 EC50 = 127.0 nM 6.90
CHEMBL491798 EC50 = 143.0 nM 6.84
CHEMBL515795 EC50 = 148.0 nM 6.83
CHEMBL521746 EC50 = 194.0 nM 6.71
CHEMBL492017 EC50 = 232.0 nM 6.63
CHEMBL476556 EC50 = 284.0 nM 6.55
CHEMBL523460 EC50 = 333.0 nM 6.48
CHEMBL489365 EC50 = 373.0 nM 6.43
CHEMBL479082 EC50 = 452.0 nM 6.34
CHEMBL490585 EC50 = 473.0 nM 6.33
CHEMBL521768 EC50 = 569.0 nM 6.25
CHEMBL490586 EC50 = 799.0 nM 6.10
CHEMBL489388 EC50 = 870.0 nM 6.06
CHEMBL490412 EC50 = 1300.0 nM 5.89
CHEMBL490409 EC50 = 3400.0 nM 5.47
CHEMBL448025 EC50 = 7790.0 nM 5.11
CHEMBL523147 EC50 = 7830.0 nM 5.11
CHEMBL522978 EC50 = 9200.0 nM 5.04
CHEMBL522280 EC50 > 30000.0 nM -
CHEMBL514557 EC50 > 30000.0 nM -
CHEMBL490410 EC50 > 30000.0 nM -
CHEMBL490411 EC50 > 30000.0 nM -
CHEMBL521797 EC50 > 30000.0 nM -
CHEMBL491804 EC50 > 30000.0 nM -
CHEMBL489366 EC50 > 30000.0 nM -