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Compound Detail

CHEMBL118266

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c1cncc(-c2csc(-c3cccnc3)n2)c1

Basic Information

ChEMBL ID CHEMBL118266
Phase Preclinical
Structure Type MOL
InChI Key ITJUUTBLPGKSOG-UHFFFAOYSA-N
6
Targets
6
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

239.3
MW (Da)
3.27
ALogP
4
HBA
0
HBD
38.7
PSA (Ų)
0.69
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 C13H9N3S
MW 239.30
Aromatic Rings 3
Heavy Atoms 17
NP-Likeness -1.76

Activity Summary

IC50 5 meas. best 8.4
Kd 1 meas. best 2.86

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Aromatase
CHEMBL1978
IC50 8.4 8.4 4.0 1
Homo sapiens
CHEMBL372
IC50 6.0 6.0 1000.0 1
MAP kinase-interacting serine/threonine-protein kinase 2
CHEMBL4204
IC50 4.7 4.7 20000.0 1
MAP kinase-interacting serine/threonine-protein kinase 1
CHEMBL4718
IC50 4.57 4.57 27000.0 1
Tyrosine-protein kinase receptor UFO
CHEMBL4895
IC50 3.52 3.52 305000.0 1
Protein polybromo-1
CHEMBL1795184
Kd 2.86 2.86 1387000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
36227159 10.1021/acs.jmedchem.2c00864 Protein polybromo-1 2
7830278 10.1021/jm00002a017 Homo sapiens 1
29525337 10.1016/j.bmc.2018.02.048 Aromatase 1
31910010 10.1021/acs.jmedchem.9b01582 MAP kinase-interacting serine/threonine-protein kinase 1 1
31910010 10.1021/acs.jmedchem.9b01582 MAP kinase-interacting serine/threonine-protein kinase 2 1
34600239 10.1016/j.bmc.2021.116437 Tyrosine-protein kinase receptor UFO 1

Data from ChEMBL 36 via Core Engine