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Compound Detail

CHEMBL1233748

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COc1cc(NC(=O)c2cccc(-n3ncc4cc(Nc5ccccc5F)ccc43)c2)cc(OC)c1OC

Basic Information

ChEMBL ID CHEMBL1233748
Phase Preclinical
Structure Type MOL
InChI Key GYQLVKWGHKBDMP-UHFFFAOYSA-N
3
Targets
6
Activities
1
Assay Types
4
PK Parameters
10
Publications
0
Known Names

Molecular Properties

512.5
MW (Da)
6.19
ALogP
7
HBA
2
HBD
86.6
PSA (Ų)
0.26
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H25FN4O4
MW 512.54
Aromatic Rings 5
Heavy Atoms 38
NP-Likeness -1.59

Activity Summary

IC50 6 meas. best 8.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mitogen-activated protein kinase 10
CHEMBL2637
IC50 8.05 8.05 9.0 2
MAP kinase p38
CHEMBL2094115
IC50 7.52 7.52 30.0 2
Mitogen-activated protein kinase 8
CHEMBL2276
IC50 7.14 7.14 73.0 2

Pharmacokinetic Data

Parameter Value Units Species
AUC 25.63 ng.hr.mL-1 Rattus norvegicus
CL 57.0 mL.min-1.kg-1 Rattus norvegicus
F 5.0 % Rattus norvegicus
T1/2 0.025 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
23518277 10.1016/j.bmcl.2013.02.082 Rattus norvegicus 4
23518277 10.1016/j.bmcl.2013.02.082 Unchecked 1
23518277 10.1016/j.bmcl.2013.02.082 Plasma 1
23518277 10.1016/j.bmcl.2013.02.082 Mitogen-activated protein kinase 8 1
23518277 10.1016/j.bmcl.2013.02.082 Brain 1
23518277 10.1016/j.bmcl.2013.02.082 MAP kinase p38 1
23518277 10.1016/j.bmcl.2013.02.082 Mitogen-activated protein kinase 10 1
25415535 10.1021/jm501212r MAP kinase p38 1
25415535 10.1021/jm501212r Mitogen-activated protein kinase 8 1
25415535 10.1021/jm501212r Mitogen-activated protein kinase 10 1

Data from ChEMBL 36 via Core Engine