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Compound Detail

CHEMBL5421749

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COc1cc2nn(CC(=O)N3CCOCC3)cc2cc1NC(=O)c1cccc(C(F)F)n1

Basic Information

ChEMBL ID CHEMBL5421749
Phase Preclinical
Structure Type MOL
InChI Key SKWDOWYVGZFBQX-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
3
PK Parameters
3
Publications
0
Known Names

Molecular Properties

445.4
MW (Da)
2.49
ALogP
7
HBA
1
HBD
98.6
PSA (Ų)
0.63
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H21F2N5O4
MW 445.43
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -1.90

Activity Summary

IC50 3 meas. best 8.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Interleukin-1 receptor-associated kinase 4
CHEMBL3778
IC50 8.1 8.1 8.0 2
Receptor-type tyrosine-protein kinase FLT3
CHEMBL1974
IC50 7.51 7.51 31.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 2.333 mL.min-1.kg-1 Rattus norvegicus
F 55.0 % Rattus norvegicus
T1/2 1.6 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
38228402 10.1021/acs.jmedchem.3c01714 ADMET 4
38228402 10.1021/acs.jmedchem.3c01714 Interleukin-1 receptor-associated kinase 4 1
38228402 10.1021/acs.jmedchem.3c01714 Receptor-type tyrosine-protein kinase FLT3 1

Data from ChEMBL 36 via Core Engine