Details of the Target

General Information of Target

Target ID LDTP05554
Target Name Epithelial discoidin domain-containing receptor 1 (DDR1)
Gene Name DDR1
Gene ID 780
Synonyms
CAK; EDDR1; NEP; NTRK4; PTK3A; RTK6; TRKE; Epithelial discoidin domain-containing receptor 1; Epithelial discoidin domain receptor 1; EC 2.7.10.1; CD167 antigen-like family member A; Cell adhesion kinase; Discoidin receptor tyrosine kinase; HGK2; Mammary carcinoma kinase 10; MCK-10; Protein-tyrosine kinase 3A; Protein-tyrosine kinase RTK-6; TRK E; Tyrosine kinase DDR; Tyrosine-protein kinase CAK; CD antigen CD167a
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MGPEALSSLLLLLLVASGDADMKGHFDPAKCRYALGMQDRTIPDSDISASSSWSDSTAAR
HSRLESSDGDGAWCPAGSVFPKEEEYLQVDLQRLHLVALVGTQGRHAGGLGKEFSRSYRL
RYSRDGRRWMGWKDRWGQEVISGNEDPEGVVLKDLGPPMVARLVRFYPRADRVMSVCLRV
ELYGCLWRDGLLSYTAPVGQTMYLSEAVYLNDSTYDGHTVGGLQYGGLGQLADGVVGLDD
FRKSQELRVWPGYDYVGWSNHSFSSGYVEMEFEFDRLRAFQAMQVHCNNMHTLGARLPGG
VECRFRRGPAMAWEGEPMRHNLGGNLGDPRARAVSVPLGGRVARFLQCRFLFAGPWLLFS
EISFISDVVNNSSPALGGTFPPAPWWPPGPPPTNFSSLELEPRGQQPVAKAEGSPTAILI
GCLVAIILLLLLIIALMLWRLHWRRLLSKAERRVLEEELTVHLSVPGDTILINNRPGPRE
PPPYQEPRPRGNPPHSAPCVPNGSALLLSNPAYRLLLATYARPPRGPGPPTPAWAKPTNT
QAYSGDYMEPEKPGAPLLPPPPQNSVPHYAEADIVTLQGVTGGNTYAVPALPPGAVGDGP
PRVDFPRSRLRFKEKLGEGQFGEVHLCEVDSPQDLVSLDFPLNVRKGHPLLVAVKILRPD
ATKNARNDFLKEVKIMSRLKDPNIIRLLGVCVQDDPLCMITDYMENGDLNQFLSAHQLED
KAAEGAPGDGQAAQGPTISYPMLLHVAAQIASGMRYLATLNFVHRDLATRNCLVGENFTI
KIADFGMSRNLYAGDYYRVQGRAVLPIRWMAWECILMGKFTTASDVWAFGVTLWEVLMLC
RAQPFGQLTDEQVIENAGEFFRDQGRQVYLSRPPACPQGLYELMLRCWSRESEQRPPFSQ
LHRFLAEDALNTV
Target Type
Patented-recorded
Target Bioclass
Enzyme
Family
Protein kinase superfamily, Tyr protein kinase family, Insulin receptor subfamily
Subcellular location
Secreted; Cell membrane
Function
Tyrosine kinase that functions as a cell surface receptor for fibrillar collagen and regulates cell attachment to the extracellular matrix, remodeling of the extracellular matrix, cell migration, differentiation, survival and cell proliferation. Collagen binding triggers a signaling pathway that involves SRC and leads to the activation of MAP kinases. Regulates remodeling of the extracellular matrix by up-regulation of the matrix metalloproteinases MMP2, MMP7 and MMP9, and thereby facilitates cell migration and wound healing. Required for normal blastocyst implantation during pregnancy, for normal mammary gland differentiation and normal lactation. Required for normal ear morphology and normal hearing. Promotes smooth muscle cell migration, and thereby contributes to arterial wound healing. Also plays a role in tumor cell invasion. Phosphorylates PTPN11.
TTD ID
T09185
Uniprot ID
Q08345
DrugMap ID
TTI1FPZ
Ensemble ID
ENST00000259875.11
HGNC ID
HGNC:2730
ChEMBL ID
CHEMBL5319

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
COLO679 SNV: p.F241L .
HCT15 SNV: p.I433V .
HEC1 SNV: p.T292M DBIA    Probe Info 
HT115 SNV: p.M130K; p.K133E .
Ishikawa (Heraklio) 02 ER SNV: p.G131D .
KARPAS299 SNV: p.D795E .
KMRC20 SNV: p.P43T .
KMS11 SNV: p.P806L .
NCIH1155 SNV: p.Q749Ter .
NCIH82 SNV: p.R444C .
NUGC3 Deletion: p.T531HfsTer122 DBIA    Probe Info 
OCIAML5 SNV: p.S360R .
OVK18 Deletion: p.P483RfsTer170 .
RKO SNV: p.A59G .
SHP77 SNV: p.M311V .
SW1783 SNV: p.R525Q .
TE4 SNV: p.R440L DBIA    Probe Info 

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 8 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
STPyne
 Probe Info  		K646(1.23)  LDD0277  [1]
OPA-S-S-alkyne
 Probe Info  		K30(1.33); K112(2.03)  LDD3494  [2]
DBIA
 Probe Info  		C778(1.59)  LDD3310  [3]
JZ128-DTB
 Probe Info  		N.A.  LDD0462  [4]
IA-alkyne
 Probe Info  		C627(0.00); C772(0.00)  LDD0162  [5]
IPM
 Probe Info  		N.A.  LDD0147  [6]
TFBX
 Probe Info  		N.A.  LDD0148  [6]
NAIA_5
 Probe Info  		N.A.  LDD2223  [7]
PAL-AfBPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
Dasatinib-CA-8PAP
 Probe Info  		N.A.  LDD0364  [8]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HEK-293T C876(1.04)  LDD1507  [9]
 LDCM0237  AC12 HEK-293T C772(1.31)  LDD1510  [9]
 LDCM0276  AC17 HEK-293T C876(1.11)  LDD1515  [9]
 LDCM0280  AC20 HEK-293T C772(0.95)  LDD1519  [9]
 LDCM0285  AC25 HEK-293T C876(0.90)  LDD1524  [9]
 LDCM0288  AC28 HEK-293T C772(1.11)  LDD1527  [9]
 LDCM0294  AC33 HEK-293T C876(0.96)  LDD1533  [9]
 LDCM0297  AC36 HEK-293T C772(1.17)  LDD1536  [9]
 LDCM0301  AC4 HEK-293T C772(1.53)  LDD1540  [9]
 LDCM0303  AC41 HEK-293T C876(1.16)  LDD1542  [9]
 LDCM0306  AC44 HEK-293T C772(1.03)  LDD1545  [9]
 LDCM0311  AC49 HEK-293T C876(0.97)  LDD1550  [9]
 LDCM0315  AC52 HEK-293T C772(1.33)  LDD1554  [9]
 LDCM0320  AC57 HEK-293T C876(1.09)  LDD1559  [9]
 LDCM0324  AC60 HEK-293T C772(1.07)  LDD1563  [9]
 LDCM0356  AKOS034007680 HEK-293T C876(0.88)  LDD1570  [9]
 LDCM0404  CL17 HEK-293T C876(1.24)  LDD1608  [9]
 LDCM0408  CL20 HEK-293T C772(1.42)  LDD1612  [9]
 LDCM0417  CL29 HEK-293T C876(1.00)  LDD1621  [9]
 LDCM0421  CL32 HEK-293T C772(1.24)  LDD1625  [9]
 LDCM0431  CL41 HEK-293T C876(1.17)  LDD1635  [9]
 LDCM0434  CL44 HEK-293T C772(1.27)  LDD1638  [9]
 LDCM0440  CL5 HEK-293T C876(1.02)  LDD1644  [9]
 LDCM0444  CL53 HEK-293T C876(1.18)  LDD1647  [9]
 LDCM0447  CL56 HEK-293T C772(1.67)  LDD1650  [9]
 LDCM0457  CL65 HEK-293T C876(1.27)  LDD1660  [9]
 LDCM0460  CL68 HEK-293T C772(1.12)  LDD1663  [9]
 LDCM0470  CL77 HEK-293T C876(1.67)  LDD1673  [9]
 LDCM0473  CL8 HEK-293T C772(1.29)  LDD1676  [9]
 LDCM0474  CL80 HEK-293T C772(1.13)  LDD1677  [9]
 LDCM0483  CL89 HEK-293T C876(0.99)  LDD1686  [9]
 LDCM0487  CL92 HEK-293T C772(1.15)  LDD1690  [9]
 LDCM0097  Dasatinib K562 N.A.  LDD0364  [8]
 LDCM0179  JZ128 PC-3 N.A.  LDD0462  [4]
 LDCM0022  KB02 22RV1 C305(2.14); C627(0.73); C778(2.44); C882(2.43)  LDD2243  [3]
 LDCM0023  KB03 22RV1 C305(2.55); C627(1.03); C778(4.01); C882(2.74)  LDD2660  [3]
 LDCM0024  KB05 COLO792 C778(1.59)  LDD3310  [3]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Discoidin domain-containing receptor 2 (DDR2) Tyr protein kinase family Q16832
Tyrosine-protein phosphatase non-receptor type 11 (PTPN11) Protein-tyrosine phosphatase family Q06124
Other
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Cytoplasmic protein NCK2 (NCK2) . O43639
Ubiquilin-2 (UBQLN2) . Q9UHD9

The Drug(s) Related To This Target

Approved
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Fostamatinib Small molecular drug DB12010
Imatinib Small molecular drug DB00619
Pralsetinib . DB15822
Investigative
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Pmid23521020c7k Small molecular drug D0BL0O
Patented
Click To Hide/Show 8 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Bdbm50080408 Small molecular drug D0Y3FD
Ng7 Small molecular drug D0GT9T
Us9156852, 83 Small molecular drug D0BW9L
Us9567304, Compound F-54 Small molecular drug D0H0GL
Us9567304, Compound N-9 Small molecular drug D00UAQ
Us9695118, 4 Small molecular drug D0ZK5P
Us9695118, 8 Small molecular drug D0DA4Y
Vapbgcraujrzpo-uhfffaoysa-n Small molecular drug D0LL1P

References

1 A Paal-Knorr agent for chemoproteomic profiling of targets of isoketals in cells. Chem Sci. 2021 Oct 15;12(43):14557-14563. doi: 10.1039/d1sc02230j. eCollection 2021 Nov 10.
Mass spectrometry data entry: PXD028270
2 A chemical proteomics approach for global mapping of functional lysines on cell surface of living cell. Nat Commun. 2024 Apr 8;15(1):2997. doi: 10.1038/s41467-024-47033-w.
Mass spectrometry data entry: PXD042888
3 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840
4 A Chemoproteomic Strategy for Direct and Proteome-Wide Covalent Inhibitor Target-Site Identification. J Am Chem Soc. 2019 Jan 9;141(1):191-203. doi: 10.1021/jacs.8b07911. Epub 2018 Dec 20.
5 SP3-FAIMS Chemoproteomics for High-Coverage Profiling of the Human Cysteinome*. Chembiochem. 2021 May 14;22(10):1841-1851. doi: 10.1002/cbic.202000870. Epub 2021 Feb 18.
Mass spectrometry data entry: PXD023056 , PXD023059 , PXD023058 , PXD023057 , PXD023060
6 Chemoproteomic Profiling by Cysteine Fluoroalkylation Reveals Myrocin G as an Inhibitor of the Nonhomologous End Joining DNA Repair Pathway. J Am Chem Soc. 2021 Dec 8;143(48):20332-20342. doi: 10.1021/jacs.1c09724. Epub 2021 Nov 24.
Mass spectrometry data entry: PXD029255
7 N-Acryloylindole-alkyne (NAIA) enables imaging and profiling new ligandable cysteines and oxidized thiols by chemoproteomics. Nat Commun. 2023 Jun 15;14(1):3564. doi: 10.1038/s41467-023-39268-w.
Mass spectrometry data entry: PXD041264
8 Streamlined Target Deconvolution Approach Utilizing a Single Photoreactive Chloroalkane Capture Tag. ACS Chem Biol. 2021 Feb 19;16(2):404-413. doi: 10.1021/acschembio.0c00987. Epub 2021 Feb 5.
9 Accelerating multiplexed profiling of protein-ligand interactions: High-throughput plate-based reactive cysteine profiling with minimal input. Cell Chem Biol. 2024 Mar 21;31(3):565-576.e4. doi: 10.1016/j.chembiol.2023.11.015. Epub 2023 Dec 19.
Mass spectrometry data entry: PXD044402