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Compound Detail

CHEMBL1795613

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CCCCc1ccc(-n2sc3ncc(-c4ccccc4)cc3c2=O)cc1

Basic Information

ChEMBL ID CHEMBL1795613
Phase Preclinical
Structure Type MOL
InChI Key CPXKVJSIEUVWNW-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

360.5
MW (Da)
5.46
ALogP
4
HBA
0
HBD
34.9
PSA (Ų)
0.47
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H20N2OS
MW 360.48
Aromatic Rings 4
Heavy Atoms 26
NP-Likeness -0.84

Activity Summary

IC50 3 meas. best 5.18

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone acetyltransferase KAT2B
CHEMBL5500
IC50 5.18 5.18 6640.0 1
Histone acetyltransferase p300
CHEMBL3784
IC50 5.08 5.08 8280.0 1
Histone acetyltransferase KAT2A
CHEMBL5501
IC50 5.06 5.06 8650.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
21353783 10.1016/j.bmc.2011.01.063 Histone acetyltransferase KAT2B 2
- 10.1039/C4MD00245H Histone acetyltransferase KAT2B 2
- 10.1039/C4MD00245H Histone acetyltransferase KAT2A 2
- 10.1039/C4MD00245H Histone acetyltransferase p300 2
21353783 10.1016/j.bmc.2011.01.063 SK-N-SH 1
21353783 10.1016/j.bmc.2011.01.063 HCT-116 1
21353783 10.1016/j.bmc.2011.01.063 MCF7 1
- 10.1039/C4MD00245H CREB-binding protein 1

Data from ChEMBL 36 via Core Engine