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Assay Detail

CHEMBL997705

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Functional
Agonist activity at human thrombopoietin receptor expressed in mouse Ba/F3 cells by kinase activation based reporter gene assay
22
Total Activities
22
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

Optimization of small molecule agonists of the thrombopoietin (Tpo) receptor derived from a benzo[a]carbazole hit scaffold.
Marsilje TH, Alper PB, Lu W, Mutnick D, Michellys PY, He Y, Karanewsky DS, Chow D, Gerken A, Lao J, Kim MJ, Seidel HM, Tian SS.
Bioorg Med Chem Lett (2008) 18 : 5259 -5262
PubMed 18783949 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 22 6.90 7.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL498173 1 7.68
CHEMBL498581 1 7.60
CHEMBL496123 1 7.58
CHEMBL496122 1 7.43
CHEMBL461101 ELTROMBOPAG 4.0 1 7.42
CHEMBL522070 1 7.29
CHEMBL496950 1 7.07
CHEMBL477195 1 6.96
CHEMBL525732 1 6.96
CHEMBL496755 1 6.94
CHEMBL525533 1 6.93
CHEMBL497793 1 6.80
CHEMBL525906 1 6.80
CHEMBL497349 1 6.75
CHEMBL495731 1 6.64
CHEMBL522391 1 6.56
CHEMBL497149 1 6.42
CHEMBL497372 1 6.35
CHEMBL526077 1 5.90
CHEMBL497582 1 5.84
CHEMBL497583 1 -
CHEMBL497348 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL498173 EC50 = 21.0 nM 7.68
CHEMBL498581 EC50 = 25.0 nM 7.60
CHEMBL496123 EC50 = 26.0 nM 7.58
CHEMBL496122 EC50 = 37.0 nM 7.43
CHEMBL461101 ELTROMBOPAG EC50 = 38.0 nM 7.42
CHEMBL522070 EC50 = 51.0 nM 7.29
CHEMBL496950 EC50 = 86.0 nM 7.07
CHEMBL477195 EC50 = 111.0 nM 6.96
CHEMBL525732 EC50 = 111.0 nM 6.96
CHEMBL496755 EC50 = 116.0 nM 6.94
CHEMBL525533 EC50 = 117.0 nM 6.93
CHEMBL497793 EC50 = 160.0 nM 6.80
CHEMBL525906 EC50 = 160.0 nM 6.80
CHEMBL497349 EC50 = 179.0 nM 6.75
CHEMBL495731 EC50 = 228.0 nM 6.64
CHEMBL522391 EC50 = 277.0 nM 6.56
CHEMBL497149 EC50 = 376.0 nM 6.42
CHEMBL497372 EC50 = 449.0 nM 6.35
CHEMBL526077 EC50 = 1260.0 nM 5.90
CHEMBL497582 EC50 = 1430.0 nM 5.84
CHEMBL497583 EC50 > 30000.0 nM -
CHEMBL497348 EC50 > 1000.0 nM -