Reaction Details |
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Target | eIF-2-alpha kinase GCN2 |
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Ligand | BDBM50072072 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1467741 (CHEMBL3412167) |
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IC50 | 5.0±n/a nM |
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Citation | Smith, AL; Andrews, KL; Beckmann, H; Bellon, SF; Beltran, PJ; Booker, S; Chen, H; Chung, YA; D'Angelo, ND; Dao, J; Dellamaggiore, KR; Jaeckel, P; Kendall, R; Labitzke, K; Long, AM; Materna-Reichelt, S; Mitchell, P; Norman, MH; Powers, D; Rose, M; Shaffer, PL; Wu, MM; Lipford, JR Discovery of 1H-pyrazol-3(2H)-ones as potent and selective inhibitors of protein kinase R-like endoplasmic reticulum kinase (PERK). J Med Chem58:1426-41 (2015) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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eIF-2-alpha kinase GCN2 |
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Name: | eIF-2-alpha kinase GCN2 |
Synonyms: | E2AK4_HUMAN | EIF2AK4 | Eukaryotic translation initiation factor 2-alpha kinase 4 | GCN2 | GCN2(Kin.Dom.2 S808G) | GCN2-like protein | KIAA1338 |
Type: | PROTEIN |
Mol. Mass.: | 186899.26 |
Organism: | Homo sapiens (Human) |
Description: | ChEMBL_1495738 |
Residue: | 1649 |
Sequence: | MAGGRGAPGRGRDEPPESYPQRQDHELQALEAIYGADFQDLRPDACGPVKEPPEINLVLY
PQGLTGEEVYVKVDLRVKCPPTYPDVVPEIELKNAKGLSNESVNLLKSRLEELAKKHCGE
VMIFELAYHVQSFLSEHNKPPPKSFHEEMLERRAQEEQQRLLEAKRKEEQEQREILHEIQ
RRKEEIKEEKKRKEMAKQERLEIASLSNQDHTSKKDPGGHRTAAILHGGSPDFVGNGKHR
ANSSGRSRRERQYSVCNSEDSPGSCEILYFNMGSPDQLMVHKGKCIGSDEQLGKLVYNAL
ETATGGFVLLYEWVLQWQKKMGPFLTSQEKEKIDKCKKQIQGTETEFNSLVKLSHPNVVR
YLAMNLKEQDDSIVVDILVEHISGVSLAAHLSHSGPIPVHQLRRYTAQLLSGLDYLHSNS
VVHKVLSASNVLVDAEGTVKITDYSISKRLADICKEDVFEQTRVRFSDNALPYKTGKKGD
VWRLGLLLLSLSQGQECGEYPVTIPSDLPADFQDFLKKCVCLDDKERWSPQQLLKHSFIN
PQPKMPLVEQSPEDSEGQDYVETVIPSNRLPSAAFFSETQRQFSRYFIEFEELQLLGKGA
FGAVIKVQNKLDGCCYAVKRIPINPASRQFRRIKGEVTLLSRLHHENIVRYYNAWIERHE
RPAGPGTPPPDSGPLAKDDRAARGQPASDTDGLDSVEAAAPPPILSSSVEWSTSGERSAS
ARFPATGPGSSDDEDDDEDEHGGVFSQSFLPASDSESDIIFDNEDENSKSQNQDEDCNEK
NGCHESEPSVTTEAVHYLYIQMEYCEKSTLRDTIDQGLYRDTVRLWRLFREILDGLAYIH
EKGMIHRDLKPVNIFLDSDDHVKIGDFGLATDHLAFSADSKQDDQTGDLIKSDPSGHLTG
MVGTALYVSPEVQGSTKSAYNQKVDLFSLGIIFFEMSYHPMVTASERIFVLNQLRDPTSP
KFPEDFDDGEHAKQKSVISWLLNHDPAKRPTATELLKSELLPPPQMEESELHEVLHHTLT
NVDGKAYRTMMAQIFSQRISPAIDYTYDSDILKGNFSIRTAKMQQHVCETIIRIFKRHGA
VQLCTPLLLPRNRQIYEHNEAALFMDHSGMLVMLPFDLRIPFARYVARNNILNLKRYCIE
RVFRPRKLDRFHPKELLECAFDIVTSTTNSFLPTAEIIYTIYEIIQEFPALQERNYSIYL
NHTMLLKAILLHCGIPEDKLSQVYIILYDAVTEKLTRREVEAKFCNLSLSSNSLCRLYKF
IEQKGDLQDLMPTINSLIKQKTGIAQLVKYGLKDLEEVVGLLKKLGIKLQVLINLGLVYK
VQQHNGIIFQFVAFIKRRQRAVPEILAAGGRYDLLIPQFRGPQALGPVPTAIGVSIAIDK
ISAAVLNMEESVTISSCDLLVVSVGQMSMSRAINLTQKLWTAGITAEIMYDWSQSQEELQ
EYCRHHEITYVALVSDKEGSHVKVKSFEKERQTEKRVLETELVDHVLQKLRTKVTDERNG
REASDNLAVQNLKGSFSNASGLFEIHGATVVPIVSVLAPEKLSASTRRRYETQVQTRLQT
SLANLHQKSSEIEILAVDLPKETILQFLSLEWDADEQAFNTTVKQLLSRLPKQRYLKLVC
DEIYNIKVEKKVSVLFLYSYRDDYYRILF
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BDBM50072072 |
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n/a |
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Name | BDBM50072072 |
Synonyms: | CHEMBL3407849 |
Type | Small organic molecule |
Emp. Form. | C33H27N5O3 |
Mol. Mass. | 541.5992 |
SMILES | CNc1ncc2ccc(Oc3cc(ccc3C)C(=O)c3c(-c4ccccc4)n(C)n(-c4ccccc4)c3=O)cc2n1 |
Structure |
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