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Target id: 1935
Nomenclature: ATR serine/threonine kinase
Abbreviated Name: ATR
Family: ATR subfamily
Gene and Protein Information ![]() |
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Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | - | 2644 | 3q23 | ATR | ATR serine/threonine kinase | |
Mouse | - | 2635 | 9 E3.3 | Atr | ataxia telangiectasia and Rad3 related | |
Rat | - | 2636 | 8q31 | Atr | ATR serine/threonine kinase |
Previous and Unofficial Names ![]() |
FRP1 | MEC1 | mitosis entry checkpoint 1, homolog (S. cerevisiae) | SCKL | SCKL1 |
Database Links ![]() |
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Alphafold | Q13535 (Hs), Q9JKK8 (Mm) |
BRENDA | 2.7.11.1 |
CATH/Gene3D | 1.10.1070.11, 1.25.10.10, 1.25.40.10 |
ChEMBL Target | CHEMBL5024 (Hs) |
Ensembl Gene | ENSG00000175054 (Hs), ENSMUSG00000032409 (Mm), ENSRNOG00000010027 (Rn) |
Entrez Gene | 545 (Hs), 245000 (Mm), 685055 (Rn) |
Human Protein Atlas | ENSG00000175054 (Hs) |
KEGG Enzyme | 2.7.11.1 |
KEGG Gene | hsa:545 (Hs), mmu:245000 (Mm), rno:685055 (Rn) |
OMIM | 601215 (Hs) |
Orphanet | ORPHA118896 (Hs) |
Pharos | Q13535 (Hs) |
RefSeq Nucleotide | NM_001184 (Hs), NM_019864 (Mm), XM_003750561 (Rn) |
RefSeq Protein | NP_001175 (Hs), NP_063917 (Mm), XP_003750609 (Rn) |
UniProtKB | Q13535 (Hs), Q9JKK8 (Mm) |
Wikipedia | ATR (Hs) |
Enzyme Reaction ![]() |
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Download all structure-activity data for this target as a CSV file
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Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Clinically-Relevant Mutations and Pathophysiology ![]() |
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1. Ahmad N, Boyall D, Charrier JD, Davis C, Davis R, Durrant S, Etxebarria I Jardi G, Fraysse D, Jiminez JM, Kay D et al.. (2014) Compounds useful as inhibitors of atr kinase. Patent number: WO2014089379A1. Assignee: Vertex Pharmaceuticals Inc.. Priority date: 07/12/2012. Publication date: 12/06/2014.
2. Berger M, Wortmann L, Buchgraber P, Lücking U, Zitzmann-Kolbe S, Wengner AM, Bader B, Bömer U, Briem H, Eis K et al.. (2021) BAY-8400: A Novel Potent and Selective DNA-PK Inhibitor which Shows Synergistic Efficacy in Combination with Targeted Alpha Therapies. J Med Chem, 64 (17): 12723-12737. [PMID:34428039]
3. Fokas E, Prevo R, Pollard JR, Reaper PM, Charlton PA, Cornelissen B, Vallis KA, Hammond EM, Olcina MM, Gillies McKenna W et al.. (2012) Targeting ATR in vivo using the novel inhibitor VE-822 results in selective sensitization of pancreatic tumors to radiation. Cell Death Dis, 3: e441. [PMID:23222511]
4. Foote KM, Blades K, Cronin A, Fillery S, Guichard SS, Hassall L, Hickson I, Jacq X, Jewsbury PJ, McGuire TM et al.. (2013) Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity. J Med Chem, 56 (5): 2125-38. [PMID:23394205]
5. Luecking UT, Lefranc J, Wengner A, Wortmann L, Schck H, Briem H, Siesmeister G, Lienau P, Schatz C, Bader B et al.. (2017) Abstract 983: Identification of potent, highly selective and orally available ATR inhibitor BAY 1895344 with favorable PK properties and promising efficacy in monotherapy and combination in preclinical tumor models. Cancer Research, 77 (13 (Supplement)). DOI: 10.1158/1538-7445.AM2017-983
6. Reaper PM, Griffiths MR, Long JM, Charrier JD, Maccormick S, Charlton PA, Golec JM, Pollard JR. (2011) Selective killing of ATM- or p53-deficient cancer cells through inhibition of ATR. Nat Chem Biol, 7 (7): 428-30. [PMID:21490603]
7. Roulston A, Zimmermann M, Papp R, Skeldon A, Pellerin C, Dumas-Bérube É, Dumais V, Dorich S, Fader LD, Fournier S et al.. (2022) RP-3500: A Novel, Potent, and Selective ATR Inhibitor that is Effective in Preclinical Models as a Monotherapy and in Combination with PARP Inhibitors. Mol Cancer Ther, 21 (2): 245-256. [PMID:34911817]
8. Toledo LI, Murga M, Zur R, Soria R, Rodriguez A, Martinez S, Oyarzabal J, Pastor J, Bischoff JR, Fernandez-Capetillo O. (2011) A cell-based screen identifies ATR inhibitors with synthetic lethal properties for cancer-associated mutations. Nat Struct Mol Biol, 18 (6): 721-7. [PMID:21552262]
9. Vendetti FP, Lau A, Schamus S, Conrads TP, O'Connor MJ, Bakkenist CJ. (2015) The orally active and bioavailable ATR kinase inhibitor AZD6738 potentiates the anti-tumor effects of cisplatin to resolve ATM-deficient non-small cell lung cancer in vivo. Oncotarget, 6 (42): 44289-305. [PMID:26517239]
10. Zenke FT, Zimmermann A, Dahmen H, Elenbaas B, Pollard J, Reaper P, Bagrodia S, Spilker ME, Amendt C, Blaukat A. Abstract 369: Antitumor activity of M4344, a potent and selective ATR inhibitor, in monotherapy and combination therapy. Accessed on 28/07/2021. Modified on 28/07/2021. cancerres.aacrjournals.org, https://cancerres.aacrjournals.org/content/79/13_Supplement/369. DOI: 10.1158/1538-7445.AM2019-369
ATR subfamily: ATR serine/threonine kinase. Last modified on 01/08/2022. Accessed on 20/05/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=1935.