activin A receptor type 1 | Type I receptor serine/threonine kinases | IUPHAR/BPS Guide to PHARMACOLOGY

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activinAreceptor|activinAreceptor,typeI|activinAreceptortypeI|ACTRI|ACVR1A|Acvrlk2|ACVRLK2|Alk-2|Alk8|serine/threonine-proteinkinasereceptorR1|SKR1|TGF-BsuperfamilyreceptortypeI|TSK-7L|TSR-I
Description:CrystalstructureofthekinasedomainoftypeIactivinreceptor(ACVR1)incomplexwithFKBP12anddorsomorphin
Description:CrystalstructureoftheACVR1(ALK2)kinaseincomplexwithcyclicalinhibitorOD36.
Downloadallstructure-activitydataforthistargetasaCSVfile

Description:InhibitoryactivityagainsthumanAKL2,determinedusingaLanthaScreenbindingassay.
EMDMilliporeKinaseProfilerTMscreen/ReactionBIOLOGyKinaseHotspotSMscreen
Ascreenprofiling158kinaseinhibitors(CalbiochemProteinKinaseInhibitorLibraryIandII,cataloguenumbers539744and539745)fortheirinhibitoryactivityat1Mand10Magainst234humanrecombinantkinasesusingtheEMDMilliporeKinaseProfilerTMservice.

Ascreenprofilingtheinhibitoryactivityof178commerciallyavailablekinaseinhibitorsat0.5Magainstapanelof300recombinantproteinkinasesusingtheReactionBiologyCorporationKinaseHotspotSMplatform.

http://www.millipore.com/techpublications/tech1/pf3036
http://www.reactionbiology.com/webapps/main/pages/kinase.aspx
Clinically-RelevantMutationsandPathophysiology
1.AnastassiADIsT,DeaconSW,DevarajanK,MaH,PetersonJR.(2011)Comprehensiveassayofkinasecatalyticactivityrevealsfeaturesofkinaseinhibitorselectivity.
2.ChaikuadA,AlfanoI,KerrG,SanvitaleCE,BoergermannJH,TriffittJT,vonDelftF,KnappS,KnausP,BullockAN.(2012)StructureofthebonemorphogeneticproteinreceptorALK2andimplicationsforfibrodysplasiaossificansprogressiva.
3.DavisMI,HuntJP,HerrgardS,CiceriP,WodickaLM,PallaresG,HockerM,TreiberDK,ZarrinkarPP.(2011)Comprehensiveanalysisofkinaseinhibitorselectivity.
4.EngersDW,FristAY,LindsleyCW,HongCC,HopkinsCR.(2013)Synthesisandstructure-activityrelationshipsofanovelandselectivebonemorphogeneticproteinreceptor(BMP)inhibitorderivedfromthepyrazolo[1.5-a]pyrimidinescaffoldofdorsomorphin:thediscoveryofML347asanALK2versusALK3selectiveMLPCNprobe.
5.MohedasAH,WangY,SanvitaleCE,CanningP,ChoiS,XingX,BullockAN,CunyGD,YuPB.(2014)Structure-activityrelationshipof3,5-diaryl-2-aminopyridineALK2inhibitorsrevealsunalteredbindingaffinityforfibrodysplasiaossificansprogressivacausingmutants.
6.MollardA,WarnerSL,FlymmGA,VankayalapatiH,BearssDJ.(2014)Jak2andalk2inhibitorsandmethodsfortheiruse.
Patentnumber:WO2014151871A9.Assignee:ToleroPharmaceuticals,Inc..Prioritydate:14/03/2013.Publicationdate:31/12/2014.7.VelaparthiU,DarneCP,WarrierJ,LiuP,RahamanH,Augustine-RauchK,ParrishK,YangZ,SwansonJ,BrownJetal..(2020)DiscoveryofBMS-986260,aPotent,Selective,andOrallyBioavailableTGFβR1InhibitorasanImmuno-oncologyAgent.
8.WodickaLM,CiceriP,DavisMI,HuntJP,FloydM,SalernoS,HuaXH,FordJM,ArmstrongRC,ZarrinkarPPetal..(2010)Activationstate-dependentbindingofsmallmoleculekinaseinhibitors:structuralinsightsfrombiochemistry.
TypeIreceptorserine/threoninekinases:activinAreceptortype1.Lastmodifiedon11/02/2020.Accessedon18/05/2020.IUPHAR/BPSGuidetoPHARMACOLOGY,http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1785.