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Compound Detail

CHEMBL4453010

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C=CC(=O)Nc1cccc2c1cc(C)n2-c1nc2c(c(NCc3ccccc3)n1)COCC2

Basic Information

ChEMBL ID CHEMBL4453010
Phase Preclinical
Structure Type MOL
InChI Key CJLYSVHXDHBDEJ-UHFFFAOYSA-N
3
Targets
4
Activities
3
Assay Types
1
PK Parameters
5
Publications
0
Known Names

Molecular Properties

439.5
MW (Da)
4.54
ALogP
6
HBA
2
HBD
81.1
PSA (Ų)
0.43
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H25N5O2
MW 439.52
Aromatic Rings 4
Heavy Atoms 33
NP-Likeness -1.06

Activity Summary

IC50 2 meas. best 7.23
EC50 1 meas. best 6.06
Ki 1 meas. best 7.58

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Transitional endoplasmic reticulum ATPase
CHEMBL1075145
Ki 7.58 7.58 26.6 1
Transitional endoplasmic reticulum ATPase
CHEMBL1075145
IC50 7.23 7.23 58.3 1
MIA PaCa-2
CHEMBL614725
EC50 6.06 6.06 880.0 1
A549
CHEMBL392
IC50 5.34 5.34 4600.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 4.31 hr -

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
30830772 10.1021/acs.jmedchem.9b00144 No relevant target 2
30606672 10.1016/j.bmc.2018.12.036 A549 1
30606672 10.1016/j.bmc.2018.12.036 Transitional endoplasmic reticulum ATPase 1
30830772 10.1021/acs.jmedchem.9b00144 Transitional endoplasmic reticulum ATPase 1
30830772 10.1021/acs.jmedchem.9b00144 MIA PaCa-2 1

Data from ChEMBL 36 via Core Engine