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Found 3 hits Enz. Inhib. hit(s) with Target = 'MER intracellular domain/EGFR extracellular domain chimera' and Ligand = 'BDBM112499'   
Target
(Institution)
LigandTarget
Links
Ligand
Links
Trg + Lig
Links
Ki
nM
ΔG°
kJ/mole
IC50
nM
Kd
nM
EC50/IC50
nM
koff
s-1
kon
M-1s-1
pHTemp
°C
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (human))
BDBM112499
PNG
(DACOMITINIB | US8623883, No. 2)
Show SMILES COc1cc2ncnc(Nc3ccc(F)c(Cl)c3)c2cc1NC(=O)\C=C\CN1CCCCC1
Show InChI InChI=1S/C24H25ClFN5O2/c1-33-22-14-20-17(24(28-15-27-20)29-16-7-8-19(26)18(25)12-16)13-21(22)30-23(32)6-5-11-31-9-3-2-4-10-31/h5-8,12-15H,2-4,9-11H2,1H3,(H,30,32)(H,27,28,29)/b6-5+
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PubMed
n/an/a 1.80n/an/an/an/an/an/a



Qilu Pharmaceutical Co, Ltd

Curated by ChEMBL


Assay Description
Inhibition of EGFR (unknown origin) by ELISA method


Eur J Med Chem 102: 445-63 (2015)

More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (human))
BDBM112499
PNG
(DACOMITINIB | US8623883, No. 2)
Show SMILES COc1cc2ncnc(Nc3ccc(F)c(Cl)c3)c2cc1NC(=O)\C=C\CN1CCCCC1
Show InChI InChI=1S/C24H25ClFN5O2/c1-33-22-14-20-17(24(28-15-27-20)29-16-7-8-19(26)18(25)12-16)13-21(22)30-23(32)6-5-11-31-9-3-2-4-10-31/h5-8,12-15H,2-4,9-11H2,1H3,(H,30,32)(H,27,28,29)/b6-5+
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Article
PubMed
n/an/a 6n/an/an/an/an/an/a



Covalution Pharma BV

Curated by ChEMBL


Assay Description
Inhibition of GST-tagged EGFR expressed in sf9 cells by ELISA


J Med Chem 55: 6243-62 (2012)

More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
MER intracellular domain/EGFR extracellular domain chimera


(Homo sapiens (human))
BDBM112499
PNG
(DACOMITINIB | US8623883, No. 2)
Show SMILES COc1cc2ncnc(Nc3ccc(F)c(Cl)c3)c2cc1NC(=O)\C=C\CN1CCCCC1
Show InChI InChI=1S/C24H25ClFN5O2/c1-33-22-14-20-17(24(28-15-27-20)29-16-7-8-19(26)18(25)12-16)13-21(22)30-23(32)6-5-11-31-9-3-2-4-10-31/h5-8,12-15H,2-4,9-11H2,1H3,(H,30,32)(H,27,28,29)/b6-5+
PDB
MMDB

KEGG

UniProtKB/SwissProt

B.MOAD
DrugBank
antibodypedia
GoogleScholar
AffyNet 
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PC cid
PC sid
PDB
UniChem

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PDB
US Patent
n/an/a 6.90n/an/an/an/an/an/a



Warner-Lambert Company LLC

US Patent


Assay Description
Inhibition of erbB tyrosine kinase activity was assessed using an ELISA-based receptor tyrosine kinase assay. Kinase reactions (50 mM HEPES, pH 7.4, ...


US Patent US8623883 (2014)

More data for this
Ligand-Target Pair
3D
3D Structure (crystal)