Reaction Details |
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Target | Serine/threonine-protein kinase haspin |
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Ligand | BDBM50603976 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_2245823 (CHEMBL5160033) |
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IC50 | 1280±n/a nM |
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Citation | Taft, BR; Yokokawa, F; Kirrane, T; Mata, AC; Huang, R; Blaquiere, N; Waldron, G; Zou, B; Simon, O; Vankadara, S; Chan, WL; Ding, M; Sim, S; Straimer, J; Guiguemde, A; Lakshminarayana, SB; Jain, JP; Bodenreider, C; Thompson, C; Lanshoeft, C; Shu, W; Fang, E; Qumber, J; Chan, K; Pei, L; Chen, YL; Schulz, H; Lim, J; Abas, SN; Ang, X; Liu, Y; Angulo-Barturen, I; Jiménez-Díaz, MB; Gamo, FJ; Crespo-Fernandez, B; Rosenthal, PJ; Cooper, RA; Tumwebaze, P; Aguiar, ACC; Campo, B; Campbell, S; Wagner, J; Diagana, TT; Sarko, C Discovery and Preclinical Pharmacology of INE963, a Potent and Fast-Acting Blood-Stage Antimalarial with a High Barrier to Resistance and Potential for Single-Dose Cures in Uncomplicated Malaria. J Med Chem65:3798-3813 (2022) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Serine/threonine-protein kinase haspin |
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Name: | Serine/threonine-protein kinase haspin |
Synonyms: | GSG2 | Germ cell-specific gene 2 protein | H-haspin | HASPIN | HASP_HUMAN | Haploid germ cell-specific nuclear protein kinase |
Type: | PROTEIN |
Mol. Mass.: | 88531.28 |
Organism: | Homo sapiens (Human) |
Description: | ChEMBL_1510616 |
Residue: | 798 |
Sequence: | MAASLPGPGSRLFRTYGAADGRRQRRPGREAAQWFPPQDRRRFFNSSGSSDASIGDPSQS
DDPDDPDDPDFPGSPVRRRRRRPGGRVPKDRPSLTVTPKRWKLRARPSLTVTPRRLGLRA
RPPQKCSTPCGPLRLPPFPSRDSGRLSPDLSVCGQPRDGDELGISASLFSSLASPCPGSP
TPRDSVISIGTSACLVAASAVPSGLHLPEVSLDRASLPCSQEEATGGAKDTRMVHQTRAS
LRSVLFGLMNSGTPEDSEFRADGKNMRESCCKRKLVVGNGPEGPGLSSTGKRRATGQDSC
QERGLQEAVRREHQEASVPKGRIVPRGIDRLERTRSSRKSKHQEATETSLLHSHRFKKGQ
KLGKDSFPTQDLTPLQNVCFWTKTRASFSFHKKKIVTDVSEVCSIYTTATSLSGSLLSEC
SNRPVMNRTSGAPSSWHSSSMYLLSPLNTLSISNKKASDAEKVYGECSQKGPVPFSHCLP
TEKLQRCEKIGEGVFGEVFQTIADHTPVAIKIIAIEGPDLVNGSHQKTFEEILPEIIISK
ELSLLSGEVCNRTEGFIGLNSVHCVQGSYPPLLLKAWDHYNSTKGSANDRPDFFKDDQLF
IVLEFEFGGIDLEQMRTKLSSLATAKSILHQLTASLAVAEASLRFEHRDLHWGNVLLKKT
SLKKLHYTLNGKSSTIPSCGLQVSIIDYTLSRLERDGIVVFCDVSMDEDLFTGDGDYQFD
IYRLMKKENNNRWGEYHPYSNVLWLHYLTDKMLKQMTFKTKCNTPAMKQIKRKIQEFHRT
MLNFSSATDLLCQHSLFK
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BDBM50603976 |
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n/a |
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Name | BDBM50603976 |
Synonyms: | CHEMBL5200247 |
Type | Small organic molecule |
Emp. Form. | C17H20FN5S |
Mol. Mass. | 345.438 |
SMILES | Cc1cc(F)ccc1-c1cnc2sc(nn12)N1CCC(C)(N)CC1 |
Structure |
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