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Compound Detail

CHEMBL1667940

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Nc1nccn2c1c(-c1ccc3ccc(-c4ccccc4)nc3c1F)nc2[C@H]1CC[C@H](C(N)=O)CC1

Basic Information

ChEMBL ID CHEMBL1667940
Phase Preclinical
Structure Type MOL
InChI Key VKQVOTWWWBKYJK-WGSAOQKQSA-N
1
Targets
1
Activities
1
Assay Types
4
PK Parameters
3
Publications
0
Known Names

Molecular Properties

480.6
MW (Da)
5.09
ALogP
6
HBA
2
HBD
112.2
PSA (Ų)
0.37
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H25FN6O
MW 480.55
Aromatic Rings 5
Heavy Atoms 36
NP-Likeness -0.91

Activity Summary

IC50 1 meas. best 8.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Insulin-like growth factor 1 receptor
CHEMBL1957
IC50 8.22 8.22 6.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 3568.0 ng.hr.mL-1 Mus musculus
CL 38.0 mL.min-1.kg-1 Mus musculus
Cmax 1900.0 nM Mus musculus
F 24.0 % Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
21251824 10.1016/j.bmcl.2010.12.094 Mus musculus 5
21251824 10.1016/j.bmcl.2010.12.094 ADMET 2
21251824 10.1016/j.bmcl.2010.12.094 Insulin-like growth factor 1 receptor 1

Data from ChEMBL 36 via Core Engine