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Compound Detail

CHEMBL336001

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Cc1ccc(-n2nc(C(C)(C)C)cc2NC(=O)Nc2ccc(OCCn3ccnc3)c3ccccc23)cc1

Basic Information

ChEMBL ID CHEMBL336001
Phase Preclinical
Structure Type MOL
InChI Key FJPAWJIHSPCJMR-UHFFFAOYSA-N
5
Targets
6
Activities
3
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

508.6
MW (Da)
6.55
ALogP
6
HBA
2
HBD
86.0
PSA (Ų)
0.26
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H32N6O2
MW 508.63
Aromatic Rings 5
Heavy Atoms 38
NP-Likeness -1.83

Activity Summary

IC50 3 meas. best 7.66
EC50 2 meas. best 7.44
Kd 1 meas. best 10.13

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mitogen-activated protein kinase 14
CHEMBL2336
Kd 10.13 10.13 0.1 1
Mitogen-activated protein kinase 14
CHEMBL260
IC50 7.66 7.66 22.0 1
Tumor necrosis factor
CHEMBL1825
EC50 7.44 6.7 36.0 2
Mitogen-activated protein kinase 12
CHEMBL4674
IC50 5.69 5.69 2050.0 1
Tyrosine-protein kinase HCK
CHEMBL3234
IC50 5.31 5.31 4937.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
14561087 10.1021/jm030121k Tumor necrosis factor 4
14561087 10.1021/jm030121k Mitogen-activated protein kinase 14 2
26800309 10.1021/acs.jmedchem.5b01029 NON-PROTEIN TARGET 2
14561087 10.1021/jm030121k Mus musculus 1
26800309 10.1021/acs.jmedchem.5b01029 Mitogen-activated protein kinase 12 1
26800309 10.1021/acs.jmedchem.5b01029 Tyrosine-protein kinase HCK 1
26800309 10.1021/acs.jmedchem.5b01029 Mitogen-activated protein kinase 14 1

Data from ChEMBL 36 via Core Engine