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Compound Detail

CHEMBL207995

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COc1cc(C=O)c(Cl)cc1NC(=O)Nc1cnc(C#N)cn1

Basic Information

ChEMBL ID CHEMBL207995
Phase Preclinical
Structure Type MOL
InChI Key YTIZDTKSGSSUMG-UHFFFAOYSA-N
16
Targets
17
Activities
2
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

331.7
MW (Da)
2.47
ALogP
6
HBA
2
HBD
117.0
PSA (Ų)
0.83
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C14H10ClN5O3
MW 331.72
Aromatic Rings 2
Heavy Atoms 23
NP-Likeness -1.50

Activity Summary

Ki 16 meas. best 7.5
IC50 1 meas. best 7.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase Chk1
CHEMBL4630
IC50 7.85 7.85 14.0 1
Serine/threonine-protein kinase Chk1
CHEMBL4630
Ki 7.5 7.5 31.6 1
Vascular endothelial growth factor receptor 3
CHEMBL1955
Ki 6.0 6.0 1000.0 1
Receptor-type tyrosine-protein kinase FLT3
CHEMBL1974
Ki 5.8 5.8 1584.9 1
Glycogen synthase kinase-3 beta
CHEMBL262
Ki 5.8 5.8 1584.9 1
Glycogen synthase kinase-3 alpha
CHEMBL2850
Ki 5.8 5.8 1584.9 1
Ribosomal protein S6 kinase alpha-3
CHEMBL2345
Ki 5.6 5.6 2511.9 1
Serine/threonine-protein kinase 3
CHEMBL4708
Ki 5.6 5.6 2511.9 1
Cyclin-dependent kinase 2
CHEMBL301
Ki 5.5 5.5 3162.3 1
Cyclin-dependent kinase 5
CHEMBL4036
Ki 5.5 5.5 3162.3 1
MAP kinase-activated protein kinase 2
CHEMBL2208
Ki 5.4 5.4 3981.1 1
Aurora kinase A
CHEMBL4722
Ki 5.4 5.4 3981.1 1
Mitogen-activated protein kinase 12
CHEMBL4674
Ki 5.4 5.4 3981.1 1
Rho-associated protein kinase 1
CHEMBL3231
Ki 5.3 5.3 5011.9 1
MAP kinase-activated protein kinase 3
CHEMBL4670
Ki 5.3 5.3 5011.9 1
Calcium/calmodulin-dependent protein kinase type 1
CHEMBL2493
Ki 5.1 5.1 7943.3 1
Serine/threonine-protein kinase D2
CHEMBL4900
Ki 5.1 5.1 7943.3 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Serine/threonine-protein kinase Chk1 IC50 = 14.0 nM 7.85 Inhibition of Chk1 16446090
Serine/threonine-protein kinase Chk1 Ki = 31.62 nM 7.5 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Vascular endothelial growth factor receptor 3 Ki = 1000.0 nM 6.0 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Glycogen synthase kinase-3 alpha Ki = 1584.89 nM 5.8 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Receptor-type tyrosine-protein kinase FLT3 Ki = 1584.89 nM 5.8 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Glycogen synthase kinase-3 beta Ki = 1584.89 nM 5.8 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Ribosomal protein S6 kinase alpha-3 Ki = 2511.89 nM 5.6 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Serine/threonine-protein kinase 3 Ki = 2511.89 nM 5.6 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Cyclin-dependent kinase 2 Ki = 3162.28 nM 5.5 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Cyclin-dependent kinase 5 Ki = 3162.28 nM 5.5 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Aurora kinase A Ki = 3981.07 nM 5.4 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
MAP kinase-activated protein kinase 2 Ki = 3981.07 nM 5.4 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Mitogen-activated protein kinase 12 Ki = 3981.07 nM 5.4 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
MAP kinase-activated protein kinase 3 Ki = 5011.87 nM 5.3 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Rho-associated protein kinase 1 Ki = 5011.87 nM 5.3 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Serine/threonine-protein kinase D2 Ki = 7943.28 nM 5.1 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Calcium/calmodulin-dependent protein kinase type 1 Ki = 7943.28 nM 5.1 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -

Literature References

PubMed DOI Target Context # Activities
16446090 10.1016/j.bmcl.2006.01.028 Serine/threonine-protein kinase Chk1 1

Data from ChEMBL 36 via Core Engine