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Compound Detail

CHEMBL465957

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O=C(Nc1nc(-c2cccc(C(F)(F)F)c2F)cs1)c1ccc(N2CCC(C(=O)O)C2)nc1

Basic Information

ChEMBL ID CHEMBL465957
Phase Preclinical
Structure Type MOL
InChI Key QHDHUEIPKWBLKG-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

480.4
MW (Da)
4.53
ALogP
6
HBA
2
HBD
95.4
PSA (Ų)
0.52
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H16F4N4O3S
MW 480.44
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -2.19

Activity Summary

EC50 1 meas. best 5.48

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Thrombopoietin receptor
CHEMBL1864
EC50 5.48 5.48 3300.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 2.5 mL.min-1.kg-1 Rattus norvegicus
F 3.0 % Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Thrombopoietin receptor EC50 = 3300.0 nM 5.48 Agonist activity at human thrombopoietin receptor transfected in mouse BAF3 cell... 19186055

Literature References

PubMed DOI Target Context # Activities
19186055 10.1016/j.bmcl.2009.01.032 No relevant target 2
19186055 10.1016/j.bmcl.2009.01.032 Rattus norvegicus 2
19186055 10.1016/j.bmcl.2009.01.032 Thrombopoietin receptor 1
19186055 10.1016/j.bmcl.2009.01.032 Caco-2 1

Data from ChEMBL 36 via Core Engine