Target
Proto-oncogene tyrosine-protein kinase Src [251-533,S345C]
Ligand
BDBM5446
Substrate
Tyr 02 Substrate Peptide
Meas. Tech.
Src IC50 Determination
pH
7.5±n/a
Temperature
296.15±n/a K
IC50
990±n/a nM
Citation
 Michalczyk, AKlüter, SRode, HBSimard, JRGrütter, CRabiller, MRauh, D Structural insights into how irreversible inhibitors can overcome drug resistance in EGFR. Bioorg Med Chem 16:3482-8 (2008) [PubMed]  Article 
Target
Name:
Proto-oncogene tyrosine-protein kinase Src [251-533,S345C]
Synonyms:
Proto-oncogene tyrosine-protein kinase Src | SRC | SRC_CHICK | Src Mutant (S345C) | cSRC-SM
Type:
Tyr protein kinase
Mol. Mass.:
32702.38
Organism:
Gallus gallus (Chicken)
Description:
Mutation of S345 to cysteine was introduced by site-directed mutagenesis and confirmed by sequence analysis.
Residue:
286
Sequence:
GHMQTQGLAKDAWEIPRESLRLEVKLGQGCFGEVWMGTWNGTTRVAIKTLKPGTMSPEAFLQEAQVMKKLRHEKLVQLYAVVSEEPIYIVTEYMSKGCLLDFLKGEMGKYLRLPQLVDMAAQIASGMAYVERMNYVHRDLRAANILVGENLVCKVADFGLARLIEDNEYTARQGAKFPIKWTAPEAALYGRFTIKSDVWSFGILLTELTTKGRVPYPGMVNREVLDQVERGYRMPCPPECPESLHDLMCQCWRKDPEERPTFEYLQAFLEDYFTSTEPQYQPGENL
  
Inhibitor
Name:
BDBM5446
Synonyms:
CHEMBL553 | ERLOTINIB HYDROCHLORIDE | Erlotinib | Erotinib | N-(3-Ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine Monohydrochloride | N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine | OSI-774 | Tarceva | US10189853, erlotinib | US10507209, Compound Erlotinib | US11524945, Compound Erlotinib | US9409845, Table 1, Compound 22: erlotinib | US9730934, Erlotinib | WO2022090481, Example erlotinib | cid_176870
Type:
Small organic molecule
Emp. Form.:
C22H23N3O4
Mol. Mass.:
393.4357
SMILES:
COCCOc1cc2ncnc(Nc3cccc(c3)C#C)c2cc1OCCOC
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Tyr 02 Substrate Peptide
Synonyms:
n/a
Type:
FRET-peptide substrate
Mol. Mass.:
358.43
Organism:
n/a
Description:
n/a
Residue:
3
Sequence:
NA