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Compound Detail

CHEMBL5178793

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Cn1cc(C(=O)Nc2sc3c(c2C#N)CCN(C(=O)c2ccc(Br)s2)C3)cn1

Basic Information

ChEMBL ID CHEMBL5178793
Phase Preclinical
Structure Type MOL
InChI Key CJGULTLBPRKTRM-UHFFFAOYSA-N
5
Targets
6
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

476.4
MW (Da)
3.63
ALogP
7
HBA
1
HBD
91.0
PSA (Ų)
0.63
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H14BrN5O2S2
MW 476.38
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -3.00

Activity Summary

IC50 5 meas. best 6.92
Kd 1 meas. best 6.44

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
MG-63
CHEMBL614347
IC50 6.92 6.92 120.0 1
143B
CHEMBL614508
IC50 6.72 6.355 190.0 2
HOS
CHEMBL614736
IC50 6.66 6.66 220.0 1
Signal transducer and activator of transcription 3
CHEMBL4026
Kd 6.44 6.44 360.0 1
Unchecked
CHEMBL612545
IC50 5.02 5.02 9500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
35476936 10.1021/acs.jmedchem.2c00004 143B 2
35476936 10.1021/acs.jmedchem.2c00004 HOS 1
35476936 10.1021/acs.jmedchem.2c00004 MG-63 1
35476936 10.1021/acs.jmedchem.2c00004 Unchecked 1
35476936 10.1021/acs.jmedchem.2c00004 Signal transducer and activator of transcription 3 1

Data from ChEMBL 36 via Core Engine