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Compound Detail

CHEMBL3394112

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COC(Cn1c(SC2CCC(C(=O)O)CC2O)nc(-c2ccc(F)cc2)c1-c1ccnc(NC(C)=O)c1)OC

Basic Information

ChEMBL ID CHEMBL3394112
Phase Preclinical
Structure Type MOL
InChI Key QRBCLMPGNQXVQO-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

558.6
MW (Da)
4.03
ALogP
9
HBA
3
HBD
135.8
PSA (Ų)
0.32
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H31FN4O6S
MW 558.63
Aromatic Rings 3
Heavy Atoms 39
NP-Likeness -0.65

Activity Summary

IC50 2 meas. best 6.87

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mitogen-activated protein kinase 14
CHEMBL260
IC50 6.87 6.87 135.0 1
Mitogen-activated protein kinase 10
CHEMBL2637
IC50 5.7 5.7 2010.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
25475894 10.1021/jm501557a Unchecked 3
25475894 10.1021/jm501557a Fibroblast growth factor receptor 3 2
25475894 10.1021/jm501557a Mitogen-activated protein kinase 10 2
25475894 10.1021/jm501557a Mitogen-activated protein kinase 14 2
25475894 10.1021/jm501557a Tyrosine-protein kinase BTK 1
25475894 10.1021/jm501557a Tyrosine-protein kinase ZAP-70 1
25475894 10.1021/jm501557a Fibroblast growth factor receptor 1 1
25475894 10.1021/jm501557a Receptor tyrosine-protein kinase erbB-4 1
25475894 10.1021/jm501557a Ephrin type-B receptor 4 1
25475894 10.1021/jm501557a Epidermal growth factor receptor 1
25475894 10.1021/jm501557a Proto-oncogene tyrosine-protein kinase Src 1
25475894 10.1021/jm501557a Casein kinase I isoform gamma-3 1
25475894 10.1021/jm501557a Tyrosine-protein kinase CSK 1
25475894 10.1021/jm501557a Cyclin-dependent kinase 4/cyclin D1 1
25475894 10.1021/jm501557a RAC-alpha serine/threonine-protein kinase 1
25475894 10.1021/jm501557a Calcium/calmodulin-dependent protein kinase type II subunit beta 1
25475894 10.1021/jm501557a ALK tyrosine kinase receptor 1
25475894 10.1021/jm501557a Aurora kinase A 1
25475894 10.1021/jm501557a Cyclin-dependent kinase 2 1
25475894 10.1021/jm501557a Tyrosine-protein kinase ABL1 1

Data from ChEMBL 36 via Core Engine