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Compound Detail

CHEMBL5190204

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CCC1CCN(c2ccc(-c3cc(F)c4c(c3)C(=O)N(C(C(=O)Nc3nccs3)c3ncn5c3CCC5)C4)cc2)CC1

Basic Information

ChEMBL ID CHEMBL5190204
Phase Preclinical
Structure Type MOL
InChI Key DTIRTKLJXKZCNC-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

584.7
MW (Da)
6.05
ALogP
7
HBA
1
HBD
83.4
PSA (Ų)
0.29
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H33FN6O2S
MW 584.72
Aromatic Rings 4
Heavy Atoms 42
NP-Likeness -1.18

Activity Summary

IC50 1 meas. best 8.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Epidermal growth factor receptor
CHEMBL203
IC50 8.4 8.4 4.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Epidermal growth factor receptor IC50 = 4.0 nM 8.4 Inhibition of EGFR L858R/T790M/C797S triple mutant (unknown origin) 34323489

Literature References

PubMed DOI Target Context # Activities
34323489 10.1021/acs.jmedchem.1c00876 Epidermal growth factor receptor 1

Data from ChEMBL 36 via Core Engine