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Target
Eukaryotic translation initiation factor 2-alpha kinase 1
Ligand
BDBM50591066
Substrate
n/a
Meas. Tech.
ChEMBL_2199073 (CHEMBL5111589)
IC50
>1000±n/a nM
Citation
 Jackson, JJ; Shibuya, GM; Ravishankar, B; Adusumilli, L; Bradford, D; Brockstedt, DG; Bucher, C; Bui, M; Cho, C; Colas, C; Cutler, G; Dukes, A; Han, X; Hu, DX; Jacobson, S; Kassner, PD; Katibah, GE; Ko, MYM; Kolhatkar, U; Leger, PR; Ma, A; Marshall, L; Maung, J; Ng, AA; Okano, A; Pookot, D; Poon, D; Ramana, C; Reilly, MK; Robles, O; Schwarz, JB; Shakhmin, AA; Shunatona, HP; Sreenivasan, R; Tivitmahaisoon, P; Xu, M; Zaw, T; Wustrow, DJ; Zibinsky, M Potent GCN2 Inhibitor Capable of Reversing MDSC-Driven T Cell Suppression Demonstrates In Vivo Efficacy as a Single Agent and in Combination with Anti-Angiogenesis Therapy. J Med Chem 65:12895-12924 (2022) [PubMed] 
Target
Name:
Eukaryotic translation initiation factor 2-alpha kinase 1
Synonyms:
E2AK1_HUMAN | EIF2AK1 | HRI | KIAA1369
Type:
PROTEIN
Mol. Mass.:
71098.55
Organism:
Homo sapiens (Human)
Description:
ChEMBL_1467744
Residue:
630
Sequence:
MQGGNSGVRKREEEGDGAGAVAAPPAIDFPAEGPDPEYDESDVPAEIQVLKEPLQQPTFPFAVANQLLLVSLLEHLSHVHEPNPLRSRQVFKLLCQTFIKMGLLSSFTCSDEFSSLRLHHNRAITHLMRSAKERVRQDPCEDISRIQKIRSREVALEAQTSRYLNEFEELAILGKGGYGRVYKVRNKLDGQYYAIKKILIKGATKTVCMKVLREVKVLAGLQHPNIVGYHTAWIEHVHVIQPRADRAAIELPSLEVLSDQEEDREQCGVKNDESSSSSIIFAEPTPEKEKRFGESDTENQNNKSVKYTTNLVIRESGELESTLELQENGLAGLSASSIVEQQLPLRRNSHLEESFTSTEESSEENVNFLGQTEAQYHLMLHIQMQLCELSLWDWIVERNKRGREYVDESACPYVMANVATKIFQELVEGVFYIHNMGIVHRDLKPRNIFLHGPDQQVKIGDFGLACTDILQKNTDWTNRNGKRTPTHTSRVGTCLYASPEQLEGSEYDAKSDMYSLGVVLLELFQPFGTEMERAEVLTGLRTGQLPESLRKRCPVQAKYIQHLTRRNSSQRPSAIQLLQSELFQNSGNVNLTLQMKIIEQEKEIAELKKQLNLLSQDKGVRDDGKDGGVG
  
Inhibitor
Name:
BDBM50591066
Synonyms:
CHEMBL5190023
Type:
Small organic molecule
Emp. Form.:
C22H23BrN8OS
Mol. Mass.:
527.44
SMILES:
CNC(=O)[C@]1(C)CC[C@H](C1)Nc1ncc2c(Br)nn(-c3ccc(cc3)-c3nnc(C)s3)c2n1 |r|
Structure:
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