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Assay Detail

CHEMBL1173858

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Functional
Agonist activity at human TPO receptor expressed in rat BaF3 cells
19
Total Activities
19
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

Structure-activity relationships and hepatic safety risks of thiazole agonists of the thrombopoietin receptor.
Antipas AS, Blumberg LC, Brissette WH, Brown MF, Casavant JM, Doty JL, Driscoll J, Harris TM, Jones CS, McCurdy SP, McElroy E, Mitton-Fry M, Munchhof MJ, Reim DA, Reiter LA, Ripp SL, Shavnya A, Smeets MI, Trevena KA.
Bioorg Med Chem Lett (2010) 20 : 4069 -4072
PubMed 20558059 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 19 6.70 7.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL523975 1 7.48
CHEMBL1170197 1 7.24
CHEMBL1172354 1 7.18
CHEMBL1172355 1 7.07
CHEMBL1170611 1 7.05
CHEMBL1171610 1 7.00
CHEMBL1171784 1 6.89
CHEMBL1171783 1 6.80
CHEMBL1170004 1 6.66
CHEMBL1172356 1 6.32
CHEMBL1169647 1 6.24
CHEMBL1170600 1 6.21
CHEMBL1170598 1 6.17
CHEMBL1171609 1 6.15
CHEMBL1169816 1 6.02
CHEMBL1169815 1 -
CHEMBL1170599 1 -
CHEMBL1170003 1 -
CHEMBL1169646 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL523975 EC50 = 33.0 nM 7.48
CHEMBL1170197 EC50 = 58.0 nM 7.24
CHEMBL1172354 EC50 = 66.0 nM 7.18
CHEMBL1172355 EC50 = 86.0 nM 7.07
CHEMBL1170611 EC50 = 89.0 nM 7.05
CHEMBL1171610 EC50 = 100.0 nM 7.00
CHEMBL1171784 EC50 = 130.0 nM 6.89
CHEMBL1171783 EC50 = 160.0 nM 6.80
CHEMBL1170004 EC50 = 220.0 nM 6.66
CHEMBL1172356 EC50 = 480.0 nM 6.32
CHEMBL1169647 EC50 = 574.0 nM 6.24
CHEMBL1170600 EC50 = 620.0 nM 6.21
CHEMBL1170598 EC50 = 670.0 nM 6.17
CHEMBL1171609 EC50 = 702.0 nM 6.15
CHEMBL1169816 EC50 = 950.0 nM 6.02
CHEMBL1169815 EC50 > 811.0 nM -
CHEMBL1170599 EC50 > 1000.0 nM -
CHEMBL1170003 EC50 > 970.0 nM -
CHEMBL1169646 EC50 > 898.0 nM -