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5AMN

The Discovery of 2-Substituted Phenol Quinazolines as Potent and Selective RET Kinase Inhibitors

Functional Information from GO Data
ChainGOidnamespacecontents
A0004672molecular_functionprotein kinase activity
A0004713molecular_functionprotein tyrosine kinase activity
A0005524molecular_functionATP binding
A0006468biological_processprotein phosphorylation
Functional Information from PDB Data
site_idAC1
Number of Residues8
DetailsBINDING SITE FOR RESIDUE FMT A 2011
ChainResidue
AGLY700
APRO701
ALEU702
ASER703
AGLN910
ALEU923
APHE924
AHIS926

site_idAC2
Number of Residues5
DetailsBINDING SITE FOR RESIDUE FMT A 2012
ChainResidue
ALEU895
ALYS907
AGLY911
AARG912
AARG873

site_idAC3
Number of Residues4
DetailsBINDING SITE FOR RESIDUE FMT A 2013
ChainResidue
AASP707
ALYS728
ALYS740
ATYR806

site_idAC4
Number of Residues1
DetailsBINDING SITE FOR RESIDUE FMT A 2014
ChainResidue
AHOH3039

site_idAC5
Number of Residues4
DetailsBINDING SITE FOR RESIDUE FMT A 2015
ChainResidue
AALA866
AVAL997
APHE998
AALA999

site_idAC6
Number of Residues1
DetailsBINDING SITE FOR RESIDUE FMT A 2016
ChainResidue
ALYS747

site_idAC7
Number of Residues3
DetailsBINDING SITE FOR RESIDUE FMT A 2017
ChainResidue
ATHR754
APHE924
AHOH3009

Functional Information from PROSITE/UniProt
site_idPS00107
Number of Residues29
DetailsPROTEIN_KINASE_ATP Protein kinases ATP-binding region signature. LGEGEFGKVVkAtafhlkgragytt.....VAVK
ChainResidueDetails
ALEU730-LYS758

site_idPS00109
Number of Residues13
DetailsPROTEIN_KINASE_TYR Tyrosine protein kinases specific active-site signature. LVHrDLAARNILV
ChainResidueDetails
ALEU870-VAL882

Functional Information from SwissProt/UniProt
site_idSWS_FT_FI1
Number of Residues1
DetailsActive site: {"description":"Proton acceptor","evidences":[{"source":"PROSITE-ProRule","id":"PRU00159","evidenceCode":"ECO:0000255"},{"source":"PROSITE-ProRule","id":"PRU10028","evidenceCode":"ECO:0000255"}]}
ChainResidueDetails

site_idSWS_FT_FI2
Number of Residues8
DetailsBinding site: {"evidences":[{"source":"PROSITE-ProRule","id":"PRU00159","evidenceCode":"ECO:0000255"},{"source":"PubMed","id":"24560924","evidenceCode":"ECO:0000305"},{"source":"PDB","id":"4CKI","evidenceCode":"ECO:0007744"}]}
ChainResidueDetails

site_idSWS_FT_FI3
Number of Residues1
DetailsBinding site: {"evidences":[{"source":"PROSITE-ProRule","id":"PRU00159","evidenceCode":"ECO:0000255"},{"source":"PubMed","id":"24560924","evidenceCode":"ECO:0000305"}]}
ChainResidueDetails

site_idSWS_FT_FI4
Number of Residues2
DetailsBinding site: {"evidences":[{"source":"PubMed","id":"20117004","evidenceCode":"ECO:0000269"},{"source":"PDB","id":"2X2M","evidenceCode":"ECO:0007744"}]}
ChainResidueDetails

site_idSWS_FT_FI5
Number of Residues1
DetailsSite: {"description":"Cleavage; by caspase-3","evidences":[{"source":"PubMed","id":"21357690","evidenceCode":"ECO:0000269"}]}
ChainResidueDetails

site_idSWS_FT_FI6
Number of Residues2
DetailsModified residue: {"description":"Phosphotyrosine; by autocatalysis","evidences":[{"source":"PubMed","id":"14711813","evidenceCode":"ECO:0000269"}]}
ChainResidueDetails

site_idSWS_FT_FI7
Number of Residues1
DetailsModified residue: {"description":"Phosphotyrosine; by autocatalysis","evidences":[{"source":"PubMed","id":"14711813","evidenceCode":"ECO:0000269"},{"source":"PubMed","id":"16928683","evidenceCode":"ECO:0000269"},{"source":"PubMed","id":"24560924","evidenceCode":"ECO:0000269"}]}
ChainResidueDetails

site_idSWS_FT_FI8
Number of Residues1
DetailsModified residue: {"description":"Phosphotyrosine; by autocatalysis","evidences":[{"source":"PubMed","id":"14711813","evidenceCode":"ECO:0000269"},{"source":"PubMed","id":"16928683","evidenceCode":"ECO:0000269"},{"source":"PubMed","id":"20117004","evidenceCode":"ECO:0000269"},{"source":"PubMed","id":"24560924","evidenceCode":"ECO:0000269"},{"source":"PubMed","id":"28846099","evidenceCode":"ECO:0000269"}]}
ChainResidueDetails

site_idSWS_FT_FI9
Number of Residues1
DetailsModified residue: {"description":"Phosphotyrosine; by autocatalysis","evidences":[{"source":"PubMed","id":"14711813","evidenceCode":"ECO:0000269"},{"source":"PubMed","id":"24560924","evidenceCode":"ECO:0000269"}]}
ChainResidueDetails

238582

PDB entries from 2025-07-09

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