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Compound Detail

CHEMBL3786567

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CC1(C)CC[C@@H](COc2cccc(-c3cn([C@H]4C[C@@H](CN5CCC5)C4)c4ncnc(N)c34)c2)O1

Basic Information

ChEMBL ID CHEMBL3786567
Phase Preclinical
Structure Type MOL
InChI Key BCTIPSBBPQBXAG-DWLFOUALSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
15
Publications
0
Known Names

Molecular Properties

461.6
MW (Da)
4.67
ALogP
7
HBA
1
HBD
78.4
PSA (Ų)
0.55
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H35N5O2
MW 461.61
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -0.18

Activity Summary

IC50 5 meas. best 8.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Insulin-like growth factor 1 receptor
CHEMBL1957
IC50 8.05 8.05 9.0 1
Insulin receptor
CHEMBL1981
IC50 7.0 7.0 100.0 1
Ephrin type-B receptor 4
CHEMBL5147
IC50 6.16 6.16 690.0 1
Proto-oncogene tyrosine-protein kinase receptor Ret
CHEMBL2041
IC50 6.01 6.01 970.0 1
Tyrosine-protein kinase Lck
CHEMBL258
IC50 5.13 5.13 7400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26951750 10.1016/j.bmcl.2016.02.074 Insulin-like growth factor 1 receptor 1
26951750 10.1016/j.bmcl.2016.02.074 Insulin receptor 1
26951750 10.1016/j.bmcl.2016.02.074 Ephrin type-B receptor 4 1
26951750 10.1016/j.bmcl.2016.02.074 Proto-oncogene tyrosine-protein kinase receptor Ret 1
26951750 10.1016/j.bmcl.2016.02.074 Tyrosine-protein kinase JAK1 1
26951750 10.1016/j.bmcl.2016.02.074 Vascular endothelial growth factor receptor 2 1
26951750 10.1016/j.bmcl.2016.02.074 Tyrosine-protein kinase Lck 1
26951750 10.1016/j.bmcl.2016.02.074 Epidermal growth factor receptor 1
26951750 10.1016/j.bmcl.2016.02.074 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform 1
26951750 10.1016/j.bmcl.2016.02.074 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform 1
26951750 10.1016/j.bmcl.2016.02.074 No relevant target 1
26951750 10.1016/j.bmcl.2016.02.074 ADMET 1
26951750 10.1016/j.bmcl.2016.02.074 Cytochrome P450 2D6 1
26951750 10.1016/j.bmcl.2016.02.074 Cytochrome P450 2C9 1
26951750 10.1016/j.bmcl.2016.02.074 Cytochrome P450 3A4 1

Data from ChEMBL 36 via Core Engine