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Compound Detail

CHEMBL487781

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Fc1ccc(-c2nn3cc(C(F)(F)F)ccc3c2-c2ccncc2)cc1

Basic Information

ChEMBL ID CHEMBL487781
Phase Preclinical
Structure Type MOL
InChI Key ORVXSLITIZZMFZ-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
4
PK Parameters
3
Publications
0
Known Names

Molecular Properties

357.3
MW (Da)
5.22
ALogP
3
HBA
0
HBD
30.2
PSA (Ų)
0.46
QED
1
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H11F4N3
MW 357.31
Aromatic Rings 4
Heavy Atoms 26
NP-Likeness -1.28

Activity Summary

IC50 1 meas. best 6.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mitogen-activated protein kinase 14
CHEMBL260
IC50 6.7 6.7 200.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 500.0 ng.hr.mL-1 Rattus norvegicus
CL 34.0 mL.min-1.kg-1 Rattus norvegicus
F 84.0 % Rattus norvegicus
T1/2 2.5 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Mitogen-activated protein kinase 14 IC50 = 200.0 nM 6.7 Inhibition of GST-fused p38alpha expressed in Escherichia coli 18818075

Literature References

PubMed DOI Target Context # Activities
18818075 10.1016/j.bmcl.2008.09.040 Rattus norvegicus 5
18818075 10.1016/j.bmcl.2008.09.040 ADMET 2
18818075 10.1016/j.bmcl.2008.09.040 Mitogen-activated protein kinase 14 1

Data from ChEMBL 36 via Core Engine