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Compound Detail

CHEMBL95284

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COc1ccc(-n2sc3ncccc3c2=O)cc1

Basic Information

ChEMBL ID CHEMBL95284
Phase Preclinical
Structure Type MOL
InChI Key AZVIMHSUSDTTCB-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

258.3
MW (Da)
2.46
ALogP
5
HBA
0
HBD
44.1
PSA (Ų)
0.71
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C13H10N2O2S
MW 258.30
Aromatic Rings 3
Heavy Atoms 18
NP-Likeness -1.22

Activity Summary

IC50 3 meas. best 5.24

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone acetyltransferase KAT2B
CHEMBL5500
IC50 5.24 5.24 5710.0 1
Bos taurus
CHEMBL613489
IC50 4.87 4.87 13500.0 2

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
7932530 10.1021/jm00045a012 Bos taurus 1
- 10.1016/S0960-894X(01)80782-4 Bos taurus 1
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

Data from ChEMBL 36 via Core Engine