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Compound Detail

CHEMBL5085698

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c1cc(CN2CCOCC2)cc(Nc2nccc(NCCc3cnc[nH]3)n2)c1

Basic Information

ChEMBL ID CHEMBL5085698
Phase Preclinical
Structure Type MOL
InChI Key FTIGOWUZQQHANO-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
14
Publications
0
Known Names

Molecular Properties

379.5
MW (Da)
2.43
ALogP
7
HBA
3
HBD
91.0
PSA (Ų)
0.55
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H25N7O
MW 379.47
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -1.74

Activity Summary

IC50 4 meas. best 6.75

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
NUAK family SNF1-like kinase 1
CHEMBL5784
IC50 6.75 6.75 176.0 1
Serine/threonine-protein kinase SIK2
CHEMBL5699
IC50 6.73 6.73 185.0 1
Activin receptor type-1
CHEMBL5903
IC50 6.27 6.27 537.0 1
Bone morphogenetic protein receptor type-1B
CHEMBL5476
IC50 5.04 5.04 9028.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
34333981 10.1021/acs.jmedchem.1c00440 Serine/threonine-protein kinase 17A 2
34333981 10.1021/acs.jmedchem.1c00440 Aurora kinase B 1
34333981 10.1021/acs.jmedchem.1c00440 MAP/microtubule affinity-regulating kinase 3 1
34333981 10.1021/acs.jmedchem.1c00440 MAP/microtubule affinity-regulating kinase 4 1
34333981 10.1021/acs.jmedchem.1c00440 Serine/threonine-protein kinase TBK1 1
34333981 10.1021/acs.jmedchem.1c00440 NUAK family SNF1-like kinase 1 1
34333981 10.1021/acs.jmedchem.1c00440 Serine/threonine-protein kinase SIK2 1
34333981 10.1021/acs.jmedchem.1c00440 Activin receptor type-1 1
34333981 10.1021/acs.jmedchem.1c00440 Bone morphogenetic protein receptor type-1B 1
34333981 10.1021/acs.jmedchem.1c00440 No relevant target 1
34333981 10.1021/acs.jmedchem.1c00440 ADMET 1
34333981 10.1021/acs.jmedchem.1c00440 Tyrosine-protein kinase JAK2 1
34333981 10.1021/acs.jmedchem.1c00440 Serine/threonine-protein kinase 17B 1
34333981 10.1021/acs.jmedchem.1c00440 BMP-2-inducible protein kinase 1

Data from ChEMBL 36 via Core Engine