6ZU8

Target information

RCSB PDB
6ZU8
Title
Crystal structure of human Brachyury G177D variant in complex with Afatinib
Method
X-RAY DIFFRACTION
Resolution
1.95
Classification
TRANSCRIPTION
Organism
Homo sapiens
Protein
T-box transcription factor T (O15178)
Year
2020
Publication Title
Crystal structure of human Brachyury G177D variant in complex with Afatinib
Abstract

Not Available

External Link
RCSB PDB





Ligand information

HET
0WN
Chain ID
A
HET Number
302
Molecular Formula
C24H25ClFN5O3
Structure
2D structure
IUPAC Name
(E)-N-[4-(3-chloro-4-fluoro-anilino)-7-[(3S)-tetrahydrofuran-3-yl]oxy-quinazolin-6-yl]-4-(dimethylamino)but-2-enamide
InChI
InChI=1S/C24H25ClFN5O3/c1-31(2)8-3-4-23(32)30-21-11-17-20(12-22(21)34-16-7-9-33-13-16)27-14-28-24(17)29-15-5-6-19(26)18(25)10-15/h3-6,10-12,14,16H,7-9,13H2,1-2H3,(H,30,32)(H,27,28,29)/b4-3+/t16-/m0/s1
InChI Key
ULXXDDBFHOBEHA-CWDCEQMOSA-N
Canonical SMILES
CN(C)C\C=C\C(=O)Nc1cc2c(Nc3ccc(F)c(Cl)c3)ncnc2cc1O[C@H]1CCOC1
Bioactivity data
CI000361

Covalent Binding

Warhead
Michael Acceptor
Reaction Mechanism
Michael Addition
Residue
CYS : 122
Residue Chain
A
Interactions
Pharmacophore Model