General Information of the Protein
Protein ID
PT01678
Protein Name
Discoidin domain-containing receptor 2
Secondarily
Protein Name
CD167 antigen-like family member B
Discoidin domain-containing receptor tyrosine kinase 2
Neurotrophic tyrosine kinase
receptor-related 3
Receptor protein-tyrosine kinase TKT
Tyrosine-protein kinase TYRO10
Gene Name
DDR2
Secondarily
Gene Name
NTRKR3
TKT
TYRO10
Sequence
MILIPRMLLVLFLLLPILSSAKAQVNPAICRYPLGMSGGQIPDEDITASSQWSESTAAKYGRLDSEEGDGAWCPEIPVEPDDLKEFLQIDLHTLHFITLVGTQGRHAGGHGIEFAPMYKINYSRDGTRWISWRNRHGKQVLDGNSNPYDIFLKDLEPPIVARFVRFIPVTDHSMNVCMRVELYGCVWLDGLVSYNAPAGQQFVLPGGSIIYLNDSVYDGAVGYSMTEGLGQLTDGVSGLDDFTQTHEYHVWPGYDYVGWRNESATNGYIEIMFEFDRIRNFTTMKVHCNNMFAKGVKIFKEVQCYFRSEASEWEPNAISFPLVLDDVNPSARFVTVPLHHRMASAIKCQYHFADTWMMFSEITFQSDAAMYNNSEALPTSPMAPTTYDPMLKVDDSNTRILIGCLVAIIFILLAIIVIILWRQFWQKMLEKASRRMLDDEMTVSLSLPSDSSMFNNNRSSSPSEQGSNSTYDRIFPLRPDYQEPSRLIRKLPEFAPGEEESGCSGVVKPVQPSGPEGVPHYAEADIVNLQGVTGGNTYSVPAVTMDLLSGKDVAVEEFPRKLLTFKEKLGEGQFGEVHLCEVEGMEKFKDKDFALDVSANQPVLVAVKMLRADANKNARNDFLKEIKIMSRLKDPNIIHLLAVCITDDPLCMITEYMENGDLNQFLSRHEPPNSSSSDVRTVSYTNLKFMATQIASGMKYLSSLNFVHRDLATRNCLVGKNYTIKIADFGMSRNLYSGDYYRIQGRAVLPIRWMSWESILLGKFTTASDVWAFGVTLWETFTFCQEQPYSQLSDEQVIENTGEFFRDQGRQTYLPQPAICPDSVYKLMLSCWRRDTKNRPSFQEIHLLLLQQGDE
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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 involved in the regulation of tissues remodeling (PubMed:30449416). It functions as a cell surface receptor for fibrillar collagen and regulates cell differentiation, remodeling of the extracellular matrix, cell migration and cell proliferation. Required for normal bone development. Regulates osteoblast differentiation and chondrocyte maturation via a signaling pathway that involves MAP kinases and leads to the activation of the transcription factor RUNX2. Regulates remodeling of the extracellular matrix by up-regulation of the collagenases MMP1, MMP2 and MMP13, and thereby facilitates cell migration and tumor cell invasion. Promotes fibroblast migration and proliferation, and thereby contributes to cutaneous wound healing.
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Uniprot ID
Primary ID:
Q16832

Secondarily ID:
Q7Z730
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HGNC ID
HGNC:2731
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
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0441015
 Compound Info 
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 = 1540 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0190068
 Compound Info 
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 = 6080 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0002778
 Compound Info 
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
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000025 , HEK-293T
 Cell Line Info 
Cell Line ID: CL000989 , NCI-H2286
 Cell Line Info 
Cell Line ID: CL000012 , Sf21
 Cell Line Info 
Cell Line ID: CL000013 , Sf9
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0005166
 Compound Info 
BMS-354825
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C22H26ClN7O2S
  7
1 IC50 = 0.4 nM
2 IC50 = 1.4 nM
3 IC50 = 2 nM
4 IC50 = 11.7 nM
5 Kd = 3 nM
6 Kd = 3.2 nM
7 Kd = 18 nM
CP0030881
 Compound Info 
SR-302
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C32H42N6O5S
  4
1 IC50 = 0.75 nM
2 IC50 = 18 nM
3 IC50 ~ 0.75 nM
4 IC50 ~ 18 nM
CP0081362
 Compound Info 
4-fluoro-2-[5-[[(1R)-2-hydroxy-1-phenylethyl]amino]-3-(3-methyl-2H-indazol-5-yl)pyridin-2-yl]phenol
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C27H23FN4O2
  1
1 IC50 = 0.8 nM
CP0002230
 Compound Info 
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
  8
1 IC50 = 2 nM
2 IC50 < 2.54 nM
3 IC50 = 55 nM
4 IC50 = 105 nM
5 Kd = 6 nM
6 Kd = 6.2 nM
7 Kd = 33 nM
8 Kd = 75 nM
CP0146667
 Compound Info 
N-[5-[[(3-fluorophenyl)carbamoylamino]methyl]-2-methylphenyl]imidazo[1,2-a]pyridine-3-carboxamide
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C23H20FN5O2
  1
1 IC50 = 3.3 nM
CP0093697
 Compound Info 
3-[[2-[3-(morpholin-4-ylmethyl)phenyl]thieno[3,2-b]pyridin-7-yl]amino]phenol
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C24H23N3O2S
  2
1 IC50 = 6 nM
2 IC50 = 145 nM
CP0002778
 Compound Info 
4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide
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C29H31N7O
  2
1 IC50 = 675 nM
2 Kd = 15 nM
CP0029924
 Compound Info 
N-[[4-(3-cyclohexylpropylcarbamoyl)phenyl]methyl]-1-phenyl-5-(trifluoromethyl)pyrazole-4-carboxamide
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C28H31F3N4O2
  1
1 IC50 ~ 220 nM
CP0030365
 Compound Info 
5-amino-N-[[4-(3-cyclohexylpropylcarbamoyl)phenyl]methyl]-1-phenylpyrazole-4-carboxamide
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C27H33N5O2
  1
1 IC50 ~ 5600 nM
CP0031151
 Compound Info 
SR-301
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C34H43N9O4S
  1
1 IC50 ~ 15500 nM
Clinical Information about the Protein
Target 1 ( Discoidin domain-containing receptor 2 (DDR2) )
Target Type Patented-recorded Target