Reaction Details Report a problem with these data
Target
Ephrin type-A receptor 8
Ligand
BDBM50357333
Substrate
n/a
Meas. Tech.
ChEMBL_787379 (CHEMBL1919258)
IC50
434±n/a nM
Citation
 Kim, KH; Maderna, A; Schnute, ME; Hegen, M; Mohan, S; Miyashiro, J; Lin, L; Li, E; Keegan, S; Lussier, J; Wrocklage, C; Nickerson-Nutter, CL; Wittwer, AJ; Soutter, H; Caspers, N; Han, S; Kurumbail, R; Dunussi-Joannopoulos, K; Douhan, J; Wissner, A Imidazo[1,5-a]quinoxalines as irreversible BTK inhibitors for the treatment of rheumatoid arthritis. Bioorg Med Chem Lett 21:6258-63 (2011) [PubMed]  Article 
Target
Name:
Ephrin type-A receptor 8
Synonyms:
EEK | EPHA8 | EPHA8_HUMAN | Ephrin receptor | Ephrin type-A receptor 8 | HEK3 | KIAA1459
Type:
PROTEIN
Mol. Mass.:
111022.09
Organism:
Homo sapiens (Human)
Description:
ChEMBL_774600
Residue:
1005
Sequence:
MAPARGRLPPALWVVTAAAAAATCVSAARGEVNLLDTSTIHGDWGWLTYPAHGWDSINEVDESFQPIHTYQVCNVMSPNQNNWLRTSWVPRDGARRVYAEIKFTLRDCNSMPGVLGTCKETFNLYYLESDRDLGASTQESQFLKIDTIAADESFTGADLGVRRLKLNTEVRSVGPLSKRGFYLAFQDIGACLAILSLRIYYKKCPAMVRNLAAFSEAVTGADSSSLVEVRGQCVRHSEERDTPKMYCSAEGEWLVPIGKCVCSAGYEERRDACVACELGFYKSAPGDQLCARCPPHSHSAAPAAQACHCDLSYYRAALDPPSSACTRPPSAPVNLISSVNGTSVTLEWAPPLDPGGRSDITYNAVCRRCPWALSRCEACGSGTRFVPQQTSLVQASLLVANLLAHMNYSFWIEAVNGVSDLSPEPRRAAVVNITTNQAAPSQVVVIRQERAGQTSVSLLWQEPEQPNGIILEYEIKYYEKDKEMQSYSTLKAVTTRATVSGLKPGTRYVFQVRARTSAGCGRFSQAMEVETGKPRPRYDTRTIVWICLTLITGLVVLLLLLICKKRHCGYSKAFQDSDEEKMHYQNGQAPPPVFLPLHHPPGKLPEPQFYAEPHTYEEPGRAGRSFTREIEASRIHIEKIIGSGDSGEVCYGRLRVPGQRDVPVAIKALKAGYTERQRRDFLSEASIMGQFDHPNIIRLEGVVTRGRLAMIVTEYMENGSLDTFLRTHDGQFTIMQLVGMLRGVGAGMRYLSDLGYVHRDLAARNVLVDSNLVCKVSDFGLSRVLEDDPDAAYTTTGGKIPIRWTAPEAIAFRTFSSASDVWSFGVVMWEVLAYGERPYWNMTNRDVISSVEEGYRLPAPMGCPHALHQLMLDCWHKDRAQRPRFSQIVSVLDALIRSPESLRATATVSRCPPPAFVRSCFDLRGGSGGGGGLTVGDWLDSIRMGRYRDHFAAGGYSSLGMVLRMNAQDVRALGITLMGHQKKILGSIQTMRAQLTSTQGPRRHL
  
Inhibitor
Name:
BDBM50357333
Synonyms:
CHEMBL1916891
Type:
Small organic molecule
Emp. Form.:
C24H25FN6O
Mol. Mass.:
432.4933
SMILES:
CN(C)C\C=C\C(=O)N(C)c1cc2c(cc1F)nc(Nc1ccccc1C)c1cncn21
Structure:
Search PDB for entries with ligand similarity: