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Compound Detail

CHEMBL243518

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Cc1ccc(Nc2nccc(Nc3ccccc3C(=O)O)n2)cc1F

Basic Information

ChEMBL ID CHEMBL243518
Phase Preclinical
Structure Type MOL
InChI Key BQWUBCRDJPIJAT-UHFFFAOYSA-N
11
Targets
11
Activities
2
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

338.3
MW (Da)
4.11
ALogP
5
HBA
3
HBD
87.1
PSA (Ų)
0.65
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H15FN4O2
MW 338.34
Aromatic Rings 3
Heavy Atoms 25
NP-Likeness -1.66

Activity Summary

Ki 10 meas. best 8.5
IC50 1 meas. best 7.03

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glycogen synthase kinase-3 beta
CHEMBL262
Ki 8.5 8.5 3.2 1
Aurora kinase B
CHEMBL2185
Ki 8.3 8.3 5.0 1
Homeodomain-interacting protein kinase 2
CHEMBL4576
Ki 8.2 8.2 6.3 1
Aurora kinase A
CHEMBL4722
Ki 7.8 7.8 15.8 1
Dual specificity protein kinase CLK4
CHEMBL4203
Ki 7.1 7.1 79.4 1
Mitogen-activated protein kinase 8
CHEMBL2276
IC50 7.03 7.03 93.0 1
Serine/threonine-protein kinase pim-1
CHEMBL2147
Ki 6.8 6.8 158.5 1
Mitogen-activated protein kinase kinase kinase kinase 4
CHEMBL6166
Ki 6.7 6.7 199.5 1
MAP kinase-interacting serine/threonine-protein kinase 2
CHEMBL4204
Ki 6.6 6.6 251.2 1
Cyclin-dependent kinase 2
CHEMBL301
Ki 6.4 6.4 398.1 1
Interleukin-1 receptor-associated kinase 4
CHEMBL3778
Ki 5.4 5.4 3981.1 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Glycogen synthase kinase-3 beta Ki = 3.162 nM 8.5 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Aurora kinase B Ki = 5.012 nM 8.3 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Homeodomain-interacting protein kinase 2 Ki = 6.31 nM 8.2 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Aurora kinase A Ki = 15.85 nM 7.8 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Dual specificity protein kinase CLK4 Ki = 79.43 nM 7.1 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Mitogen-activated protein kinase 8 IC50 = 93.0 nM 7.03 Inhibition at human JNK1 at 1uM 17107797
Serine/threonine-protein kinase pim-1 Ki = 158.49 nM 6.8 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Mitogen-activated protein kinase kinase kinase kinase 4 Ki = 199.53 nM 6.7 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
MAP kinase-interacting serine/threonine-protein kinase 2 Ki = 251.19 nM 6.6 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Cyclin-dependent kinase 2 Ki = 398.11 nM 6.4 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -
Interleukin-1 receptor-associated kinase 4 Ki = 3981.07 nM 5.4 PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member na... -

Literature References

PubMed DOI Target Context # Activities
17107797 10.1016/j.bmcl.2006.10.093 Mitogen-activated protein kinase 8 1

Data from ChEMBL 36 via Core Engine