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Compound Detail

CHEMBL5200385

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CC(=O)N[C@H]1CC[C@H](n2c(=O)c(-c3ccccc3Cl)cc3ccc(Nc4ccc(N5CCN(C)CC5)c(C)c4)cc32)CC1

Basic Information

ChEMBL ID CHEMBL5200385
Phase Preclinical
Structure Type MOL
InChI Key LMRRNKPYCBBKDT-XQESHEEFSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

598.2
MW (Da)
6.75
ALogP
6
HBA
2
HBD
69.6
PSA (Ų)
0.26
QED
2
Ro5 Violations
6
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C35H40ClN5O2
MW 598.19
Aromatic Rings 4
Heavy Atoms 43
NP-Likeness -1.16

Activity Summary

IC50 1 meas. best 7.32

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Epidermal growth factor receptor
CHEMBL203
IC50 7.32 7.32 47.8 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Epidermal growth factor receptor IC50 = 47.8 nM 7.32 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