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Compound Detail

CHEMBL3695569

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COCC(=O)Nc1cc(Oc2ccc(NC(=O)Nc3cc(C(C)(C)C)nn3-c3ccc(C)cc3)c3ccccc23)ccn1

Basic Information

ChEMBL ID CHEMBL3695569
Phase Preclinical
Structure Type MOL
InChI Key AVUUHIYJPTWYNX-UHFFFAOYSA-N
8
Targets
51
Activities
2
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

578.7
MW (Da)
7.05
ALogP
7
HBA
3
HBD
119.4
PSA (Ų)
0.18
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 C33H34N6O4
MW 578.67
Aromatic Rings 5
Heavy Atoms 43
NP-Likeness -1.64

Activity Summary

IC50 32 meas. best 8.52
Kd 19 meas. best 9.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mitogen-activated protein kinase 14
CHEMBL260
Kd 9.0 9.0 1.0 2
Unchecked
CHEMBL612545
Kd 9.0 8.31 1.0 2
Tyrosine-protein kinase HCK
CHEMBL3234
IC50 8.52 8.52 3.0 1
Proto-oncogene tyrosine-protein kinase Src
CHEMBL267
Kd 8.4 8.4 4.0 3
Proto-oncogene tyrosine-protein kinase Src
CHEMBL267
IC50 8.3 8.3 5.0 6
Tyrosine-protein kinase HCK
CHEMBL3234
Kd 8.3 8.3 5.0 2
Mitogen-activated protein kinase 12
CHEMBL4674
Kd 8.3 8.3 5.0 3
Tyrosine-protein kinase SYK
CHEMBL2599
Kd 8.05 8.05 9.0 3
Mitogen-activated protein kinase 14
CHEMBL260
IC50 7.92 7.92 12.0 7
Unchecked
CHEMBL612545
IC50 7.92 7.92 12.0 1
Glycogen synthase kinase-3 beta
CHEMBL262
Kd 7.62 7.62 24.0 1
Tyrosine-protein kinase SYK
CHEMBL2599
IC50 7.38 7.38 42.0 5
Glycogen synthase kinase-3 alpha
CHEMBL2850
IC50 7.35 7.35 45.0 6
Glycogen synthase kinase-3 alpha
CHEMBL2850
Kd 6.75 6.75 180.0 3
Mitogen-activated protein kinase 12
CHEMBL4674
IC50 6.46 6.46 344.0 6

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Mitogen-activated protein kinase 14 Kd = 1.0 nM 9.0 Enzyme Inhibition: p38 MAPKα: The inhibitory activities of test compounds agains... -
Mitogen-activated protein kinase 14 Kd = 1.0 nM 9.0 p38 MAPKalpha Enzyme Inhibition: The inhibitory activities of test compounds aga... -
Unchecked Kd = 1.0 nM 9.0 p38 MAPKα Enzyme Inhibition: The inhibitory activities of test compounds against... -
Tyrosine-protein kinase HCK IC50 = 3.0 nM 8.52 Fluorescence Resonance Energy Transfer (FRET) Assay: The enzyme inhibitory activ... -
Proto-oncogene tyrosine-protein kinase Src Kd = 4.0 nM 8.4 c-Src and Syk Enzyme Inhibition: The inhibitory activities of compounds of the i... -
Proto-oncogene tyrosine-protein kinase Src Kd = 4.0 nM 8.4 c-Src and Syk Enzyme Inhibition: The inhibitory activities of compounds of the i... -
Proto-oncogene tyrosine-protein kinase Src Kd = 4.0 nM 8.4 Enzyme Inhibition: c-Src and Syk: The inhibitory activities of compounds of the ... -
Tyrosine-protein kinase HCK Kd = 5.0 nM 8.3 c-Src and Syk Enzyme Inhibition: The inhibitory activities of compounds of the i... -
Proto-oncogene tyrosine-protein kinase Src IC50 = 5.0 nM 8.3 c-Src and Syk Enzyme Inhibition: The inhibitory activities of compounds of the i... -
Proto-oncogene tyrosine-protein kinase Src IC50 = 5.0 nM 8.3 c-Src Enzyme Inhibition 1: The inhibitory activities of compounds of the inventi... -
Proto-oncogene tyrosine-protein kinase Src IC50 = 5.0 nM 8.3 c-Src and Syk Enzyme Inhibition: The inhibitory activities of compounds of the i... -
Proto-oncogene tyrosine-protein kinase Src IC50 = 5.0 nM 8.3 Enzyme Inhibition: c-Src and Syk: The inhibitory activities of compounds of the ... -
Proto-oncogene tyrosine-protein kinase Src IC50 = 5.0 nM 8.3 c-Src and Syk Enzyme Inhibition Assay: The inhibitory activities of compounds of... -
Mitogen-activated protein kinase 12 Kd = 5.0 nM 8.3 Enzyme Inhibition: p38 MAPKγ: The inhibitory activities of compounds of the inve... -
Proto-oncogene tyrosine-protein kinase Src IC50 = 5.0 nM 8.3 Fluorescence Resonance Energy Transfer (FRET) Assay: The enzyme inhibitory activ... -
Mitogen-activated protein kinase 12 Kd = 5.0 nM 8.3 p38 MAPKgamma Enzyme Inhibition: The inhibitory activities of compounds of the i... -
Tyrosine-protein kinase HCK Kd = 5.0 nM 8.3 c-Src and Syk Enzyme Inhibition: The inhibitory activities of compounds of the i... -
Mitogen-activated protein kinase 12 Kd = 5.0 nM 8.3 p38 MAPKγ Enzyme Inhibition: The inhibitory activities of compounds of the inven... -
Tyrosine-protein kinase SYK Kd = 9.0 nM 8.05 Enzyme Inhibition: c-Src and Syk: The inhibitory activities of compounds of the ... -
Tyrosine-protein kinase SYK Kd = 9.0 nM 8.05 c-Src and Syk Enzyme Inhibition: The inhibitory activities of compounds of the i... -

Data from ChEMBL 36 via Core Engine