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Compound Detail

CHEMBL1822135

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O=C(Cc1cccc2ncc(C(F)(F)F)cc12)Nc1scc(Br)c1-c1ncn[nH]1

Basic Information

ChEMBL ID CHEMBL1822135
Phase Preclinical
Structure Type MOL
InChI Key FXBNFLKLXHFULB-UHFFFAOYSA-N
3
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

482.3
MW (Da)
5.04
ALogP
5
HBA
2
HBD
83.6
PSA (Ų)
0.43
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H11BrF3N5OS
MW 482.29
Aromatic Rings 4
Heavy Atoms 29
NP-Likeness -1.96

Activity Summary

IC50 4 meas. best 7.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mitogen-activated protein kinase 8
CHEMBL2276
IC50 7.68 7.68 21.0 1
Mitogen-activated protein kinase 10
CHEMBL2637
IC50 7.28 7.28 52.0 1
Mitogen-activated protein kinase 9
CHEMBL4179
IC50 6.79 6.045 164.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
21813278 10.1016/j.bmcl.2011.06.100 Liver microsomes 2
21813278 10.1016/j.bmcl.2011.06.100 Mitogen-activated protein kinase 10 1
21813278 10.1016/j.bmcl.2011.06.100 Mitogen-activated protein kinase 8 1
21813278 10.1016/j.bmcl.2011.06.100 Mitogen-activated protein kinase 9 1
21813278 10.1016/j.bmcl.2011.06.100 Liver 1

Data from ChEMBL 36 via Core Engine