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Compound Detail

CHEMBL4460205

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

Basic Information

ChEMBL ID CHEMBL4460205
Phase Preclinical
Structure Type MOL
InChI Key PMGFXYJSBWCPQR-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

451.5
MW (Da)
4.38
ALogP
6
HBA
2
HBD
81.1
PSA (Ų)
0.44
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H25N5O2
MW 451.53
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -0.94

Activity Summary

EC50 1 meas. best 6.22
Ki 1 meas. best 7.49

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Transitional endoplasmic reticulum ATPase
CHEMBL1075145
Ki 7.49 7.49 32.3 1
MIA PaCa-2
CHEMBL614725
EC50 6.22 6.22 600.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 16.2 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
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