General Information of the Protein
Protein ID
PT02113
Protein Name
Epithelial discoidin domain-containing receptor 1
Secondarily
Protein Name
CD167 antigen-like family member A
Cell adhesion kinase
Discoidin receptor tyrosine kinase
HGK2
Mammary carcinoma kinase 10
Protein-tyrosine kinase 3A
Protein-tyrosine kinase RTK-6
TRK E
Tyrosine kinase DDR
Tyrosine-protein kinase CAK
Gene Name
DDR1
Secondarily
Gene Name
CAK
EDDR1
NEP
NTRK4
PTK3A
RTK6
TRKE
Sequence
MGPEALSSLLLLLLVASGDADMKGHFDPAKCRYALGMQDRTIPDSDISASSSWSDSTAARHSRLESSDGDGAWCPAGSVFPKEEEYLQVDLQRLHLVALVGTQGRHAGGLGKEFSRSYRLRYSRDGRRWMGWKDRWGQEVISGNEDPEGVVLKDLGPPMVARLVRFYPRADRVMSVCLRVELYGCLWRDGLLSYTAPVGQTMYLSEAVYLNDSTYDGHTVGGLQYGGLGQLADGVVGLDDFRKSQELRVWPGYDYVGWSNHSFSSGYVEMEFEFDRLRAFQAMQVHCNNMHTLGARLPGGVECRFRRGPAMAWEGEPMRHNLGGNLGDPRARAVSVPLGGRVARFLQCRFLFAGPWLLFSEISFISDVVNNSSPALGGTFPPAPWWPPGPPPTNFSSLELEPRGQQPVAKAEGSPTAILIGCLVAIILLLLLIIALMLWRLHWRRLLSKAERRVLEEELTVHLSVPGDTILINNRPGPREPPPYQEPRPRGNPPHSAPCVPNGSALLLSNPAYRLLLATYARPPRGPGPPTPAWAKPTNTQAYSGDYMEPEKPGAPLLPPPPQNSVPHYAEADIVTLQGVTGGNTYAVPALPPGAVGDGPPRVDFPRSRLRFKEKLGEGQFGEVHLCEVDSPQDLVSLDFPLNVRKGHPLLVAVKILRPDATKNARNDFLKEVKIMSRLKDPNIIRLLGVCVQDDPLCMITDYMENGDLNQFLSAHQLEDKAAEGAPGDGQAAQGPTISYPMLLHVAAQIASGMRYLATLNFVHRDLATRNCLVGENFTIKIADFGMSRNLYAGDYYRVQGRAVLPIRWMAWECILMGKFTTASDVWAFGVTLWEVLMLCRAQPFGQLTDEQVIENAGEFFRDQGRQVYLSRPPACPQGLYELMLRCWSRESEQRPPFSQLHRFLAEDALNTV
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
TK protein kinase group
>
Tyrosine protein kinase DDR family
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 (By similarity). Promotes smooth muscle cell migration, and thereby contributes to arterial wound healing. Also plays a role in tumor cell invasion. Phosphorylates PTPN11.
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Uniprot ID
Primary ID:
Q08345

Secondarily ID:
B5A975
B5A976
B7Z2K0
Q14196
Q16562
Q2L6H3
Q4LE50
Q5ST11
Q5ST12
Q6NSK4
Q9UD35
Q9UD36
Q9UD37
Q9UD86
Q9UDL2
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Ensembl ID
ENSG00000204580
HGNC ID
HGNC:2730
Subcellular Location
Cell membrane
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000077 , Ba/F3
Compound ID Compound Name Compound Formula
CP0441015
N-[4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]-3-[[3-[(E)-2-pyridin-2-ylethenyl]-1H-indazol-6-yl]sulfanyl]propanamide
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C30H31F3N6OS
 1
1
GI50 = 1360 nM
   TI
   LI
   LO
   TS
CP0190068
N-[4-methyl-3-[1-(6-methylpyridine-3-carbonyl)piperidin-4-yl]oxyphenyl]-4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)benzamide
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C33H38F3N5O3
 1
1
GI50 = 9770 nM
   TI
   LI
   LO
   TS
CP0002778
4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide
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C29H31N7O
 1
1
GI50 > 10000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0005166
BMS-354825
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C22H26ClN7O2S
 3
1 IC50 = 0.5 nM
2 IC50 = 4.8 nM
3 Kd = 0.69 nM
CP0552454
4-[(4-ethylpiperazin-1-yl)methyl]-N-[4-methyl-3-[(2-oxo-1,3-dihydroindol-6-yl)oxy]phenyl]-3-(trifluoromethyl)benzamide
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C30H31F3N4O3
 1
1 IC50 = 10.2 nM
CP0343839
2-[2-(4-acetamidophenyl)-4-amino-7-oxo-6H-pyrazolo[3,4-d]pyridazin-3-yl]-3-methyl-N-[3-(trifluoromethyl)phenyl]-1-benzofuran-6-carboxamide
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C30H22F3N7O4
 1
1 IC50 = 10.6 nM
CP0030881
SR-302
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C32H42N6O5S
 4
1 IC50 = 23 nM
2 IC50 = 53.3 nM
3 IC50 ~ 23 nM
4 IC50 ~ 53.3 nM
CP0002230
4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]benzamide
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C28H22F3N7O
 3
1 IC50 = 32.6 nM
2 IC50 = 43 nM
3 Kd = 1.1 nM
CP0137641
1-[4-chloro-3-(trifluoromethyl)phenyl]-3-(5-oxo-6-pyridin-4-ylpyrido[2,3-b][1,5]benzoxazepin-9-yl)urea
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C25H15ClF3N5O3
 1
1 IC50 = 180 nM
CP0002778
4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide
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C29H31N7O
 4
1 IC50 = 337 nM
2 IC50 = 31000 nM
3 Kd = 0.7 nM
4 Kd = 0.7943 nM
CP0030365
5-amino-N-[[4-(3-cyclohexylpropylcarbamoyl)phenyl]methyl]-1-phenylpyrazole-4-carboxamide
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C27H33N5O2
 1
1 IC50 ~ 3000 nM
CP0029924
N-[[4-(3-cyclohexylpropylcarbamoyl)phenyl]methyl]-1-phenyl-5-(trifluoromethyl)pyrazole-4-carboxamide
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C28H31F3N4O2
 1
1 IC50 ~ 13000 nM
CP0031151
SR-301
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C34H43N9O4S
 1
1 IC50 ~ 21900 nM
Clinical Information about the Protein
Target 1 ( Epithelial discoidin domain receptor 1 (DDR1) )
Target Type Patented-recorded Target