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Compound Detail

CHEMBL1170611

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O=C(Nc1nc(-c2ccc(F)c(C(F)(F)F)c2)c(F)s1)c1cnc(N2CCC(C(=O)O)CC2)c(Cl)c1

Basic Information

ChEMBL ID CHEMBL1170611
Phase Preclinical
Structure Type MOL
InChI Key WPHUOGQIPMUSNW-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
4
Publications
0
Known Names

Molecular Properties

546.9
MW (Da)
5.71
ALogP
6
HBA
2
HBD
95.4
PSA (Ų)
0.40
QED
2
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H16ClF5N4O3S
MW 546.91
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness -1.83

Activity Summary

EC50 1 meas. best 7.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Thrombopoietin receptor
CHEMBL1864
EC50 7.05 7.05 89.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 2.79 mL.min-1.kg-1 Rattus norvegicus
F 73.0 % Rattus norvegicus
T1/2 1.67 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Thrombopoietin receptor EC50 = 89.0 nM 7.05 Agonist activity at human TPO receptor expressed in rat BaF3 cells 20558059

Literature References

PubMed DOI Target Context # Activities
22533875 10.1021/jm300343m Rattus norvegicus 4
20558059 10.1016/j.bmcl.2010.05.087 Mus musculus 2
20558059 10.1016/j.bmcl.2010.05.087 Rattus norvegicus 2
20558059 10.1016/j.bmcl.2010.05.087 Thrombopoietin receptor 1

Data from ChEMBL 36 via Core Engine