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Compound Detail

CHEMBL5095186

KSQ-4279
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COc1ncnc(C2CC2)c1-c1ncc2cnn(Cc3ccc(-c4nc(C(F)(F)F)cn4C(C)C)cc3)c2n1

Basic Information

ChEMBL ID CHEMBL5095186
Name KSQ-4279
Phase Preclinical
Structure Type MOL
InChI Key KCBWAFJCKVKYHO-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

534.5
MW (Da)
5.68
ALogP
9
HBA
0
HBD
96.4
PSA (Ų)
0.27
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H25F3N8O
MW 534.55
Aromatic Rings 5
Heavy Atoms 39
NP-Likeness -1.29

Activity Summary

IC50 3 meas. best 7.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Ubiquitin carboxyl-terminal hydrolase 1
CHEMBL1795087
IC50 7.96 7.61 11.0 2
Ubiquitin carboxyl-terminal hydrolase 1/WD repeat-containing protein 48
CHEMBL3430885
IC50 7.67 7.67 21.3 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
39190802 10.1021/acs.jmedchem.4c01184 Ubiquitin carboxyl-terminal hydrolase 1 11
38889606 10.1016/j.ejmech.2024.116568 Ubiquitin carboxyl-terminal hydrolase 1/WD repeat-containing protein 48 3
38955347 10.1021/acs.jmedchem.4c00113 Ubiquitin carboxyl-terminal hydrolase 1 1
38889606 10.1016/j.ejmech.2024.116568 MDA-MB-436 1
39190802 10.1021/acs.jmedchem.4c01184 Unchecked 1
39190802 10.1021/acs.jmedchem.4c01184 Ubiquitin carboxyl-terminal hydrolase 12 1
39190802 10.1021/acs.jmedchem.4c01184 Ubiquitin carboxyl-terminal hydrolase 46 1
39190802 10.1021/acs.jmedchem.4c01184 Ubiquitin carboxyl-terminal hydrolase 11 1

Data from ChEMBL 36 via Core Engine