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Compound Detail

CHEMBL4758092

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COc1cc(OCc2ccnc(Nc3cn[nH]c3)n2)cc2sc(N[C@H]3CCCC[C@@H]3O)nc12

Basic Information

ChEMBL ID CHEMBL4758092
Phase Preclinical
Structure Type MOL
InChI Key DKQKTLVTAWREHY-IRXDYDNUSA-N
2
Targets
2
Activities
1
Assay Types
2
PK Parameters
2
Publications
0
Known Names

Molecular Properties

467.6
MW (Da)
3.86
ALogP
10
HBA
4
HBD
130.1
PSA (Ų)
0.31
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H25N7O3S
MW 467.56
Aromatic Rings 4
Heavy Atoms 33
NP-Likeness -1.48

Activity Summary

IC50 2 meas. best 9.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Macrophage colony-stimulating factor 1 receptor
CHEMBL1844
IC50 9.1 9.1 0.8 1
Macrophage colony-stimulating factor 1 receptor
CHEMBL5570
IC50 8.15 8.15 7.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 120.0 mL.min-1.kg-1 Rattus norvegicus
CL 32.0 mL.min-1.kg-1 Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
32787110 10.1021/acs.jmedchem.0c00936 Macrophage colony-stimulating factor 1 receptor 2
32787110 10.1021/acs.jmedchem.0c00936 ADMET 2

Data from ChEMBL 36 via Core Engine