BDBM13216 BMS-354825::CHEMBL1421::DASATINIB::N-(2-Chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide::N-(2-chloro-6-methylphenyl)-2-({6-[4-(2-hydroxyethyl)piperazin-1-yl]-2-methylpyrimidin-4-yl}amino)-1,3-thiazole-5-carboxamide::US10294227, Code Dasatinib::US20230348453, Compound A8::cid_3062316::med.21724, Compound Dasatinib

SMILES Cc1nc(Nc2ncc(s2)C(=O)Nc2c(C)cccc2Cl)cc(n1)N1CCN(CCO)CC1

InChI Key InChIKey=ZBNZXTGUTAYRHI-UHFFFAOYSA-N

Data  11 KI  187 IC50  891 Kd  5 EC50

PDB links: 21 PDB IDs match this monomer.

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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 11 hits for monomerid = 13216   

TargetDiscoidin domain-containing receptor 2(Homo sapiens (Human))
Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences

LigandPNGBDBM13216(BMS-354825 | CHEMBL1421 | DASATINIB | N-(2-Chloro-...)
Affinity DataIC50:  36.3nMpH: 7.5 T: 2°CAssay Description:The effects of compounds on the kinases DDR1 and DDR2 were assessed by using a LanthaScreen Eu kinase activity assay technology (Invitrogen, Carlsbad...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDiscoidin domain-containing receptor 2(Homo sapiens (Human))
Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences

LigandPNGBDBM13216(BMS-354825 | CHEMBL1421 | DASATINIB | N-(2-Chloro-...)
Affinity DataIC50:  0.400nMAssay Description:Inhibition of wild type DDR2 (unknown origin) preincubated for 30 mins before substrate addition by FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDiscoidin domain-containing receptor 2(Homo sapiens (Human))
Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences

LigandPNGBDBM13216(BMS-354825 | CHEMBL1421 | DASATINIB | N-(2-Chloro-...)
Affinity DataKd:  3nMAssay Description:Binding affinity to wild type DDR2 (unknown origin) by FLiK assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDiscoidin domain-containing receptor 2(Homo sapiens (Human))
Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences

LigandPNGBDBM13216(BMS-354825 | CHEMBL1421 | DASATINIB | N-(2-Chloro-...)
Affinity DataKd:  18nMAssay Description:Binding affinity to human acrylodan-labeled N-terminal His-tagged DDR2 (558 to 855 aa) by FLiK assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDiscoidin domain-containing receptor 2(Homo sapiens (Human))
Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences

LigandPNGBDBM13216(BMS-354825 | CHEMBL1421 | DASATINIB | N-(2-Chloro-...)
Affinity DataIC50:  1.40nMAssay Description:Inhibition of DDR2 (unknown origin) assessed as reduction in collagen-induced DDR2 activationMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDiscoidin domain-containing receptor 2(Homo sapiens (Human))
Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences

LigandPNGBDBM13216(BMS-354825 | CHEMBL1421 | DASATINIB | N-(2-Chloro-...)
Affinity DataIC50:  2nMAssay Description:Inhibition of DDR2 (unknown origin) after 1 hr by time resolved fluorescence methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDiscoidin domain-containing receptor 2(Homo sapiens (Human))
Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences

LigandPNGBDBM13216(BMS-354825 | CHEMBL1421 | DASATINIB | N-(2-Chloro-...)
Affinity DataKd:  3.20nMAssay Description:Binding constant for DDR2 kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDiscoidin domain-containing receptor 2(Homo sapiens (Human))
Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences

LigandPNGBDBM13216(BMS-354825 | CHEMBL1421 | DASATINIB | N-(2-Chloro-...)
Affinity DataIC50:  12nMAssay Description:Inhibition of DDR2 (unknown origin) using fluorescein-labeled poly GAT as substrate incubated for 1 hr prior to substrate addition measured after 1 h...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDiscoidin domain-containing receptor 2(Homo sapiens (Human))
Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences

LigandPNGBDBM13216(BMS-354825 | CHEMBL1421 | DASATINIB | N-(2-Chloro-...)
Affinity DataKd:  3.20nMAssay Description:Binding constant for DDR2 kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDiscoidin domain-containing receptor 2(Homo sapiens (Human))
Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences

LigandPNGBDBM13216(BMS-354825 | CHEMBL1421 | DASATINIB | N-(2-Chloro-...)
Affinity DataIC50:  1.40nMAssay Description:Inhibition of DDR2 (unknown origin) using poly (Glu, Tyr) 4:1 substrate after 60 mins by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDiscoidin domain-containing receptor 2(Homo sapiens (Human))
Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences

LigandPNGBDBM13216(BMS-354825 | CHEMBL1421 | DASATINIB | N-(2-Chloro-...)
Affinity DataIC50:  1.40nMAssay Description:Inhibition of DDR2 (unknown origin) using poly (Glu, Tyr) 4:1 substrate after 60 mins by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed