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Target
Ubiquitin-like modifier-activating enzyme 1
Ligand
BDBM329816
Substrate
n/a
Meas. Tech.
Ubiquitin Activating Enzyme (UAE) HTRF Assay
IC50
<10±n/a nM
Citation
 Afroze, R; Bharathan, IT; Ciavarri, JP; Fleming, PE; Gaulin, JL; Girard, M; Langston, SP; Soucy, F; Wong, T; Ye, Y Pyrazolopyrimidinyl inhibitors of ubiquitin-activating enzyme US Patent  US10202389 Publication Date 2/12/2019 
Target
Name:
Ubiquitin-like modifier-activating enzyme 1
Synonyms:
A1S9T | UBA1 | UBA1_HUMAN | UBE1
Type:
PROTEIN
Mol. Mass.:
117834.03
Organism:
Homo sapiens (Human)
Description:
ChEMBL_827630
Residue:
1058
Sequence:
MSSSPLSKKRRVSGPDPKPGSNCSPAQSVLSEVPSVPTNGMAKNGSEADIDEGLYSRQLYVLGHEAMKRLQTSSVLVSGLRGLGVEIAKNIILGGVKAVTLHDQGTAQWADLSSQFYLREEDIGKNRAEVSQPRLAELNSYVPVTAYTGPLVEDFLSGFQVVVLTNTPLEDQLRVGEFCHNRGIKLVVADTRGLFGQLFCDFGEEMILTDSNGEQPLSAMVSMVTKDNPGVVTCLDEARHGFESGDFVSFSEVQGMVELNGNQPMEIKVLGPYTFSICDTSNFSDYIRGGIVSQVKVPKKISFKSLVASLAEPDFVVTDFAKFSRPAQLHIGFQALHQFCAQHGRPPRPRNEEDAAELVALAQAVNARALPAVQQNNLDEDLIRKLAYVAAGDLAPINAFIGGLAAQEVMKACSGKFMPIMQWLYFDALECLPEDKEVLTEDKCLQRQNRYDGQVAVFGSDLQEKLGKQKYFLVGAGAIGCELLKNFAMIGLGCGEGGEIIVTDMDTIEKSNLNRQFLFRPWDVTKLKSDTAAAAVRQMNPHIRVTSHQNRVGPDTERIYDDDFFQNLDGVANALDNVDARMYMDRRCVYYRKPLLESGTLGTKGNVQVVIPFLTESYSSSQDPPEKSIPICTLKNFPNAIEHTLQWARDEFEGLFKQPAENVNQYLTDPKFVERTLRLAGTQPLEVLEAVQRSLVLQRPQTWADCVTWACHHWHTQYSNNIRQLLHNFPPDQLTSSGAPFWSGPKRCPHPLTFDVNNPLHLDYVMAAANLFAQTYGLTGSQDRAAVATFLQSVQVPEFTPKSGVKIHVSDQELQSANASVDDSRLEELKATLPSPDKLPGFKMYPIDFEKDDDSNFHMDFIVAASNLRAENYDIPSADRHKSKLIAGKIIPAIATTTAAVVGLVCLELYKVVQGHRQLDSYKNGFLNLALPFFGFSEPLAAPRHQYYNQEWTLWDRFEVQGLQPNGEEMTLKQFLDYFKTEHKLEITMLSQGVSMLYSFFMPAAKLKERLDQPMTEIVSRVSKRKLGRHVRALVLELCCNDESGEDVEVPYVRYTIR
  
Inhibitor
Name:
BDBM329816
Synonyms:
(rac)-((1R,2R,3S,4R)-4-(2-(1H-indol-2-yl)pyrazolo[1,5-a]pyrimidin-7-ylamino)-2,3- | US10202389, Compound I-024 | US9663525, Compound I-024 | US9796725, Compound I-024
Type:
Small organic molecule
Emp. Form.:
C20H22N6O5S
Mol. Mass.:
458.491
SMILES:
NS(=O)(=O)OC[C@H]1C[C@@H](Nc2ccnc3cc(nn23)-c2cc3ccccc3[nH]2)[C@H](O)[C@@H]1O |r|
Structure:
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