Reaction Details Report a problem with these data
Target
Receptor tyrosine-protein kinase erbB-4
Ligand
BDBM112499
Substrate
n/a
Meas. Tech.
ChEMBL_1613065 (CHEMBL3854865)
IC50
74±n/a nM
Citation
 Smaill, JB; Gonzales, AJ; Spicer, JA; Lee, H; Reed, JE; Sexton, K; Althaus, IW; Zhu, T; Black, SL; Blaser, A; Denny, WA; Ellis, PA; Fakhoury, S; Harvey, PJ; Hook, K; McCarthy, FO; Palmer, BD; Rivault, F; Schlosser, K; Ellis, T; Thompson, AM; Trachet, E; Winters, RT; Tecle, H; Bridges, A Tyrosine Kinase Inhibitors. 20. Optimization of Substituted Quinazoline and Pyrido[3,4-d]pyrimidine Derivatives as Orally Active, Irreversible Inhibitors of the Epidermal Growth Factor Receptor Family. J Med Chem 59:8103-24 (2016) [PubMed]  Article 
Target
Name:
Receptor tyrosine-protein kinase erbB-4
Synonyms:
ERBB4 | ERBB4_HUMAN | Epidermal growth factor receptor | Epidermal growth factor receptor 4 (ERBB4) | ErbB-4 (HER4) Tyrosine Kinase | HER4 | Proto-oncogene c-ErbB-4 | Proto-oncogene-like protein c-ErbB-4 | Receptor protein-tyrosine kinase erbB-4 | Tyrosine kinase-type cell surface receptor HER4 | Tyrosine kinase-type cell surface receptor HER4 (HER4)
Type:
Protein
Mol. Mass.:
146803.56
Organism:
Homo sapiens (Human)
Description:
Q15303
Residue:
1308
Sequence:
MKPATGLWVWVSLLVAAGTVQPSDSQSVCAGTENKLSSLSDLEQQYRALRKYYENCEVVMGNLEITSIEHNRDLSFLRSVREVTGYVLVALNQFRYLPLENLRIIRGTKLYEDRYALAIFLNYRKDGNFGLQELGLKNLTEILNGGVYVDQNKFLCYADTIHWQDIVRNPWPSNLTLVSTNGSSGCGRCHKSCTGRCWGPTENHCQTLTRTVCAEQCDGRCYGPYVSDCCHRECAGGCSGPKDTDCFACMNFNDSGACVTQCPQTFVYNPTTFQLEHNFNAKYTYGAFCVKKCPHNFVVDSSSCVRACPSSKMEVEENGIKMCKPCTDICPKACDGIGTGSLMSAQTVDSSNIDKFINCTKINGNLIFLVTGIHGDPYNAIEAIDPEKLNVFRTVREITGFLNIQSWPPNMTDFSVFSNLVTIGGRVLYSGLSLLILKQQGITSLQFQSLKEISAGNIYITDNSNLCYYHTINWTTLFSTINQRIVIRDNRKAENCTAEGMVCNHLCSSDGCWGPGPDQCLSCRRFSRGRICIESCNLYDGEFREFENGSICVECDPQCEKMEDGLLTCHGPGPDNCTKCSHFKDGPNCVEKCPDGLQGANSFIFKYADPDRECHPCHPNCTQGCNGPTSHDCIYYPWTGHSTLPQHARTPLIAAGVIGGLFILVIVGLTFAVYVRRKSIKKKRALRRFLETELVEPLTPSGTAPNQAQLRILKETELKRVKVLGSGAFGTVYKGIWVPEGETVKIPVAIKILNETTGPKANVEFMDEALIMASMDHPHLVRLLGVCLSPTIQLVTQLMPHGCLLEYVHEHKDNIGSQLLLNWCVQIAKGMMYLEERRLVHRDLAARNVLVKSPNHVKITDFGLARLLEGDEKEYNADGGKMPIKWMALECIHYRKFTHQSDVWSYGVTIWELMTFGGKPYDGIPTREIPDLLEKGERLPQPPICTIDVYMVMVKCWMIDADSRPKFKELAAEFSRMARDPQRYLVIQGDDRMKLPSPNDSKFFQNLLDEEDLEDMMDAEEYLVPQAFNIPPPIYTSRARIDSNRSEIGHSPPPAYTPMSGNQFVYRDGGFAAEQGVSVPYRAPTSTIPEAPVAQGATAEIFDDSCCNGTLRKPVAPHVQEDSSTQRYSADPTVFAPERSPRGELDEEGYMTPMRDKPKQEYLNPVEENPFVSRRKNGDLQALDNPEYHNASNGPPKAEDEYVNEPLYLNTFANTLGKAEYLKNNILSMPEKAKKAFDNPDYWNHSLPPRSTLQHPDYLQEYSTKYFYKQNGRIRPIVAENPEYLSEFSLKPGTVLPPPPYRHRNTVV
  
Inhibitor
Name:
BDBM112499
Synonyms:
DACOMITINIB | US8623883, No. 2 | WO2022090481, Example dacomitinib
Type:
Small organic molecule
Emp. Form.:
C24H25ClFN5O2
Mol. Mass.:
469.939
SMILES:
COc1cc2ncnc(Nc3ccc(F)c(Cl)c3)c2cc1NC(=O)\C=C\CN1CCCCC1
Structure:
Search PDB for entries with ligand similarity: