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5IU2

Discovery of imidazoquinolines as a novel class of potent, selective and in vivo efficacious COT kinase inhibitors

Functional Information from GO Data
ChainGOidnamespacecontents
A0004672molecular_functionprotein kinase activity
A0005524molecular_functionATP binding
A0006468biological_processprotein phosphorylation
B0004672molecular_functionprotein kinase activity
B0005524molecular_functionATP binding
B0006468biological_processprotein phosphorylation
Functional Information from PDB Data
site_idAC1
Number of Residues22
Detailsbinding site for residue 6DA A 401
ChainResidue
ATRP132
AGLY210
AGLY213
ASER214
AGLU217
ASER257
AASN258
AVAL260
AVAL269
AASP270
AHOH502
ALEU134
AHOH539
AHOH542
AHOH556
APHE149
AGLY150
AVAL152
AALA165
ALYS167
AMET207
AGLU208

site_idAC2
Number of Residues22
Detailsbinding site for residue 6DA B 401
ChainResidue
BTRP132
BLEU134
BPHE149
BGLY150
BVAL152
BALA165
BLYS167
BMET207
BGLU208
BALA209
BGLY210
BGLY213
BSER214
BGLU217
BSER257
BASN258
BVAL260
BVAL269
BASP270
BHOH506
BHOH508
BHOH534

Functional Information from PROSITE/UniProt
site_idPS00108
Number of Residues13
DetailsPROTEIN_KINASE_ST Serine/Threonine protein kinases active-site signature. ViHhDIKpsNIVF
ChainResidueDetails
AVAL249-PHE261

Functional Information from SwissProt/UniProt
site_idSWS_FT_FI1
Number of Residues2
DetailsActive site: {"description":"Proton acceptor","evidences":[{"source":"PROSITE-ProRule","id":"PRU00159","evidenceCode":"ECO:0000255"},{"source":"PROSITE-ProRule","id":"PRU10027","evidenceCode":"ECO:0000255"}]}
ChainResidueDetails

site_idSWS_FT_FI2
Number of Residues18
DetailsBinding site: {"evidences":[{"source":"PROSITE-ProRule","id":"PRU00159","evidenceCode":"ECO:0000255"}]}
ChainResidueDetails

site_idSWS_FT_FI3
Number of Residues2
DetailsModified residue: {"description":"Phosphothreonine","evidences":[{"source":"PubMed","id":"17472361","evidenceCode":"ECO:0000269"}]}
ChainResidueDetails

site_idSWS_FT_FI4
Number of Residues2
DetailsModified residue: {"description":"Phosphoserine","evidences":[{"source":"PubMed","id":"23186163","evidenceCode":"ECO:0007744"},{"source":"PubMed","id":"24275569","evidenceCode":"ECO:0007744"}]}
ChainResidueDetails

site_idSWS_FT_FI5
Number of Residues2
DetailsModified residue: {"description":"Phosphothreonine","evidences":[{"source":"PubMed","id":"15466476","evidenceCode":"ECO:0000269"},{"source":"PubMed","id":"15699325","evidenceCode":"ECO:0000269"}]}
ChainResidueDetails

242842

PDB entries from 2025-10-08

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