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Compound Detail

CHEMBL4558932

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C#CC(=O)Nc1cccc2c1cc(C)n2-c1nc2c(c(NCc3ccccc3)n1)CCCC2

Basic Information

ChEMBL ID CHEMBL4558932
Phase Preclinical
Structure Type MOL
InChI Key RKCSJJATGAWCBK-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

435.5
MW (Da)
4.79
ALogP
5
HBA
2
HBD
71.8
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 C27H25N5O
MW 435.53
Aromatic Rings 4
Heavy Atoms 33
NP-Likeness -1.15

Activity Summary

EC50 1 meas. best 6.88
Ki 1 meas. best 7.42

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Transitional endoplasmic reticulum ATPase
CHEMBL1075145
Ki 7.42 7.42 37.9 1
MIA PaCa-2
CHEMBL614725
EC50 6.88 6.88 131.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.21 hr -

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
30830772 10.1021/acs.jmedchem.9b00144 Transitional endoplasmic reticulum ATPase 3
30830772 10.1021/acs.jmedchem.9b00144 No relevant target 2
30830772 10.1021/acs.jmedchem.9b00144 MIA PaCa-2 1

Data from ChEMBL 36 via Core Engine