Found 8 hits for monomerid = 50072033 Target/Host (Institution) | Ligand | Target/Host Links | Ligand Links | Trg + Lig Links | Ki nM | ΔG° kcal/mole | IC50 nM | Kd nM | EC50/IC50 nM | koff s-1 | kon M-1s-1 | pH | Temp °C |
Eukaryotic translation initiation factor 2-alpha kinase 3
(Homo sapiens (Human)) | BDBM50072033
(CHEMBL3407859)Show SMILES Cc1ccc(C(=O)c2c(-c3ccccc3)n(C)n(-c3ccccc3)c2=O)c(N)c1-c1ccc2nc(CF)sc2c1 Show InChI InChI=1S/C32H25FN4O2S/c1-19-13-15-23(29(34)27(19)21-14-16-24-25(17-21)40-26(18-33)35-24)31(38)28-30(20-9-5-3-6-10-20)36(2)37(32(28)39)22-11-7-4-8-12-22/h3-17H,18,34H2,1-2H3 | PDB
UniProtKB/SwissProt
antibodypedia GoogleScholar AffyNet
| CHEMBL PC cid PC sid UniChem
Patents
Similars
| Article PubMed
| n/a | n/a | 53 | n/a | n/a | n/a | n/a | n/a | n/a |
Amgen Inc.
Curated by ChEMBL
| Assay Description Inhibition of GCN2 phosphorylation in human U2OS cells preincubated for 1 hr followed by drug wash out and incubated for 2 hrs by MSD assay |
J Med Chem 58: 1426-41 (2015)
Article DOI: 10.1021/jm5017494 BindingDB Entry DOI: 10.7270/Q27W6DWN |
More data for this Ligand-Target Pair | |
Eukaryotic translation initiation factor 2-alpha kinase 3
(Homo sapiens (Human)) | BDBM50072033
(CHEMBL3407859)Show SMILES Cc1ccc(C(=O)c2c(-c3ccccc3)n(C)n(-c3ccccc3)c2=O)c(N)c1-c1ccc2nc(CF)sc2c1 Show InChI InChI=1S/C32H25FN4O2S/c1-19-13-15-23(29(34)27(19)21-14-16-24-25(17-21)40-26(18-33)35-24)31(38)28-30(20-9-5-3-6-10-20)36(2)37(32(28)39)22-11-7-4-8-12-22/h3-17H,18,34H2,1-2H3 | PDB
UniProtKB/SwissProt
antibodypedia GoogleScholar AffyNet
| CHEMBL PC cid PC sid UniChem
Patents
Similars
| Article PubMed
| n/a | n/a | 3.70E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
Amgen Inc.
Curated by ChEMBL
| Assay Description Inhibition of GCN2 in amino acid starved human HT1080 cells assessed as inhibition of CHoP mRNA expression preincubated for 1 hr followed by 2 hrs in... |
J Med Chem 58: 1426-41 (2015)
Article DOI: 10.1021/jm5017494 BindingDB Entry DOI: 10.7270/Q27W6DWN |
More data for this Ligand-Target Pair | |
Eukaryotic translation initiation factor 2-alpha kinase 3
(Homo sapiens (Human)) | BDBM50072033
(CHEMBL3407859)Show SMILES Cc1ccc(C(=O)c2c(-c3ccccc3)n(C)n(-c3ccccc3)c2=O)c(N)c1-c1ccc2nc(CF)sc2c1 Show InChI InChI=1S/C32H25FN4O2S/c1-19-13-15-23(29(34)27(19)21-14-16-24-25(17-21)40-26(18-33)35-24)31(38)28-30(20-9-5-3-6-10-20)36(2)37(32(28)39)22-11-7-4-8-12-22/h3-17H,18,34H2,1-2H3 | PDB
UniProtKB/SwissProt
antibodypedia GoogleScholar AffyNet
| CHEMBL PC cid PC sid UniChem
Patents
Similars
| Article PubMed
| n/a | n/a | 6 | n/a | n/a | n/a | n/a | n/a | n/a |
Amgen Inc.
Curated by ChEMBL
| Assay Description Inhibition of human N-terminal His-tagged PERK expressed in Escherichia coli using AviTag C-terminal, N-terminal His-tagged eIF2alpha (3 to 315) as s... |
J Med Chem 58: 1426-41 (2015)
Article DOI: 10.1021/jm5017494 BindingDB Entry DOI: 10.7270/Q27W6DWN |
More data for this Ligand-Target Pair | |
Eukaryotic translation initiation factor 2-alpha kinase 3
(Homo sapiens (Human)) | BDBM50072033
(CHEMBL3407859)Show SMILES Cc1ccc(C(=O)c2c(-c3ccccc3)n(C)n(-c3ccccc3)c2=O)c(N)c1-c1ccc2nc(CF)sc2c1 Show InChI InChI=1S/C32H25FN4O2S/c1-19-13-15-23(29(34)27(19)21-14-16-24-25(17-21)40-26(18-33)35-24)31(38)28-30(20-9-5-3-6-10-20)36(2)37(32(28)39)22-11-7-4-8-12-22/h3-17H,18,34H2,1-2H3 | PDB
UniProtKB/SwissProt
antibodypedia GoogleScholar AffyNet
| CHEMBL PC cid PC sid UniChem
Patents
Similars
| Article PubMed
| n/a | n/a | 2.10E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
Amgen Inc.
Curated by ChEMBL
| Assay Description Inhibition of PERK in human HT1080 cells assessed as inhibition of thapsigargin-induced CHoP mRNA expression preincubated for 1 hr followed by thapsi... |
J Med Chem 58: 1426-41 (2015)
Article DOI: 10.1021/jm5017494 BindingDB Entry DOI: 10.7270/Q27W6DWN |
More data for this Ligand-Target Pair | |
Serine/threonine-protein kinase B-raf
(Homo sapiens (Human)) | BDBM50072033
(CHEMBL3407859)Show SMILES Cc1ccc(C(=O)c2c(-c3ccccc3)n(C)n(-c3ccccc3)c2=O)c(N)c1-c1ccc2nc(CF)sc2c1 Show InChI InChI=1S/C32H25FN4O2S/c1-19-13-15-23(29(34)27(19)21-14-16-24-25(17-21)40-26(18-33)35-24)31(38)28-30(20-9-5-3-6-10-20)36(2)37(32(28)39)22-11-7-4-8-12-22/h3-17H,18,34H2,1-2H3 | PDB MMDB
NCI pathway Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD DrugBank antibodypedia GoogleScholar AffyNet
| CHEMBL PC cid PC sid UniChem
Patents
Similars
| Article PubMed
| n/a | n/a | >1.00E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
Amgen Inc.
Curated by ChEMBL
| Assay Description Inhibition of recombinant BRAF V600E kinase domain mutant (unknown origin) |
J Med Chem 58: 1426-41 (2015)
Article DOI: 10.1021/jm5017494 BindingDB Entry DOI: 10.7270/Q27W6DWN |
More data for this Ligand-Target Pair | |
Eukaryotic translation initiation factor 2-alpha kinase 3
(Homo sapiens (Human)) | BDBM50072033
(CHEMBL3407859)Show SMILES Cc1ccc(C(=O)c2c(-c3ccccc3)n(C)n(-c3ccccc3)c2=O)c(N)c1-c1ccc2nc(CF)sc2c1 Show InChI InChI=1S/C32H25FN4O2S/c1-19-13-15-23(29(34)27(19)21-14-16-24-25(17-21)40-26(18-33)35-24)31(38)28-30(20-9-5-3-6-10-20)36(2)37(32(28)39)22-11-7-4-8-12-22/h3-17H,18,34H2,1-2H3 | PDB
UniProtKB/SwissProt
antibodypedia GoogleScholar AffyNet
| CHEMBL PC cid PC sid UniChem
Patents
Similars
| Article PubMed
| n/a | n/a | 65 | n/a | n/a | n/a | n/a | n/a | n/a |
Amgen Inc.
Curated by ChEMBL
| Assay Description Inhibition of doxycycline-inducible T-REx-PERK-FLAG (unknown origin) autophosphorylation tranfected in human HT1080 cells after 1 hr by sandwich ELIS... |
J Med Chem 58: 1426-41 (2015)
Article DOI: 10.1021/jm5017494 BindingDB Entry DOI: 10.7270/Q27W6DWN |
More data for this Ligand-Target Pair | |
Eukaryotic translation initiation factor 2-alpha kinase 3
(Homo sapiens (Human)) | BDBM50072033
(CHEMBL3407859)Show SMILES Cc1ccc(C(=O)c2c(-c3ccccc3)n(C)n(-c3ccccc3)c2=O)c(N)c1-c1ccc2nc(CF)sc2c1 Show InChI InChI=1S/C32H25FN4O2S/c1-19-13-15-23(29(34)27(19)21-14-16-24-25(17-21)40-26(18-33)35-24)31(38)28-30(20-9-5-3-6-10-20)36(2)37(32(28)39)22-11-7-4-8-12-22/h3-17H,18,34H2,1-2H3 | PDB
UniProtKB/SwissProt
antibodypedia GoogleScholar AffyNet
| CHEMBL PC cid PC sid UniChem
Patents
Similars
| Article PubMed
| n/a | n/a | n/a | n/a | 170 | n/a | n/a | n/a | n/a |
Amgen Inc.
Curated by ChEMBL
| Assay Description Inhibition of PERK-mediated protein synthesis in human U2OS cells harboring thapsigargin-induced ER stress assessed as incorporation of L-azidohomoal... |
J Med Chem 58: 1426-41 (2015)
Article DOI: 10.1021/jm5017494 BindingDB Entry DOI: 10.7270/Q27W6DWN |
More data for this Ligand-Target Pair | |
Eukaryotic translation initiation factor 2-alpha kinase 4
(Homo sapiens (Human)) | BDBM50072033
(CHEMBL3407859)Show SMILES Cc1ccc(C(=O)c2c(-c3ccccc3)n(C)n(-c3ccccc3)c2=O)c(N)c1-c1ccc2nc(CF)sc2c1 Show InChI InChI=1S/C32H25FN4O2S/c1-19-13-15-23(29(34)27(19)21-14-16-24-25(17-21)40-26(18-33)35-24)31(38)28-30(20-9-5-3-6-10-20)36(2)37(32(28)39)22-11-7-4-8-12-22/h3-17H,18,34H2,1-2H3 | PDB MMDB
KEGG
UniProtKB/SwissProt
B.MOAD antibodypedia GoogleScholar AffyNet
| CHEMBL PC cid PC sid UniChem
Patents
Similars
| Article PubMed
| n/a | n/a | 310 | n/a | n/a | n/a | n/a | n/a | n/a |
Amgen Inc.
Curated by ChEMBL
| Assay Description Inhibition of human C-terminal His-tagged GCN2 expressed in Escherichia coli using AviTag C-terminal, N-terminal His-tagged eIF2alpha (3 to 315) as s... |
J Med Chem 58: 1426-41 (2015)
Article DOI: 10.1021/jm5017494 BindingDB Entry DOI: 10.7270/Q27W6DWN |
More data for this Ligand-Target Pair | |