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Assay Detail

CHEMBL1019476

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Agonist activity at human thrombopoietin receptor transfected in mouse BAF3 cells assessed as stimulation of beta lactamase activity incubated in dark up to 1 hr
20
Total Activities
20
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

The identification of orally bioavailable thrombopoietin agonists.
Munchhof MJ, Antipas AS, Blumberg LC, Brissette WH, Brown MF, Casavant JM, Doty JL, Driscoll J, Harris TM, Wolf-Gouveia LA, Jones CS, Li Q, Linde RG, Lira PD, Marfat A, McElroy E, Mitton-Fry M, McCurdy SP, Reiter LA, Ripp SL, Shavnya A, Thomasco LM, Trevena KA.
Bioorg Med Chem Lett (2009) 19 : 1428 -1430
PubMed 19186055 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 20 7.04 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL429295 1 8.15
CHEMBL455654 1 8.00
CHEMBL462874 1 7.55
CHEMBL523975 1 7.48
CHEMBL516993 1 7.47
CHEMBL461174 1 7.37
CHEMBL459474 1 7.30
CHEMBL459687 1 7.25
CHEMBL524116 1 7.24
CHEMBL490096 1 6.89
CHEMBL461974 1 6.87
CHEMBL461975 1 6.86
CHEMBL462144 1 6.60
CHEMBL489309 1 6.53
CHEMBL523097 1 6.37
CHEMBL518057 1 6.31
CHEMBL465957 1 5.48
CHEMBL455445 1 -
CHEMBL463814 1 -
CHEMBL461100 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL429295 EC50 = 7.0 nM 8.15
CHEMBL455654 EC50 = 10.0 nM 8.00
CHEMBL462874 EC50 = 28.0 nM 7.55
CHEMBL523975 EC50 = 33.0 nM 7.48
CHEMBL516993 EC50 = 34.0 nM 7.47
CHEMBL461174 EC50 = 43.0 nM 7.37
CHEMBL459474 EC50 = 50.0 nM 7.30
CHEMBL459687 EC50 = 56.0 nM 7.25
CHEMBL524116 EC50 = 57.0 nM 7.24
CHEMBL490096 EC50 = 129.0 nM 6.89
CHEMBL461974 EC50 = 134.0 nM 6.87
CHEMBL461975 EC50 = 138.0 nM 6.86
CHEMBL462144 EC50 = 253.0 nM 6.60
CHEMBL489309 EC50 = 294.0 nM 6.53
CHEMBL523097 EC50 = 430.0 nM 6.37
CHEMBL518057 EC50 = 485.0 nM 6.31
CHEMBL465957 EC50 = 3300.0 nM 5.48
CHEMBL455445 EC50 > 10000.0 nM -
CHEMBL463814 EC50 > 1000.0 nM -
CHEMBL461100 EC50 > 1000.0 nM -