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Compound Detail

CHEMBL269696

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CC(CO)/N=C(\N)c1c(O)nsc1Nc1ccc(Oc2cc(F)ccc2Cl)c(Cl)c1

Basic Information

ChEMBL ID CHEMBL269696
Phase Preclinical
Structure Type MOL
InChI Key ZIMAVVDCVUMUBP-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
2
Publications
0
Known Names

Molecular Properties

471.3
MW (Da)
4.92
ALogP
7
HBA
4
HBD
113.0
PSA (Ų)
0.29
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H17Cl2FN4O3S
MW 471.34
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -1.34

Activity Summary

IC50 1 meas. best 7.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dual specificity mitogen-activated protein kinase kinase 1
CHEMBL3587
IC50 7.52 7.52 30.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC - - Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dual specificity mitogen-activated protein kinase kinase 1 IC50 = 30.0 nM 7.52 Inhibition of MEK-1 activity 16934458

Literature References

PubMed DOI Target Context # Activities
16934458 10.1016/j.bmcl.2006.08.048 Dual specificity mitogen-activated protein kinase kinase 1 2
16934458 10.1016/j.bmcl.2006.08.048 Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine