Pharos : Ligand Details - J495KZAV9P7K

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Ligand Summary

Ligand Structure

chemical structure image

Synonyms & Links

Name: EXEL-2880/GSK-1363089

PubChem: 42642645

Guide to Pharmacology: 5679

ChEMBL: CHEMBL1230609

LyCHI: J495KZAV9P7K

Target Activities

MET

Tclin

Hepatocyte growth factor receptor

35 Activities

Items per page:

1 – 10 of 35

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
IC50	7.85		Bioorg. Med. Chem., (2016) 24:4:812	26810712

IC50	7.85		Bioorg. Med. Chem., (2016) 24:8:1749	26964675

IC50	8.4		Eur J Med Chem, (2016) 120:None:37	27187857

IC50	8.49		Bioorg. Med. Chem., (2016) 24:16:3353	27068889

IC50	8.72		Bioorg. Med. Chem. Lett., (2016) 26:7:1680	26923692

IC50	8.73		Bioorg. Med. Chem., (2014) 22:4:1236	24485123

IC50	8.73		Bioorg. Med. Chem. Lett., (2016) 26:7:1794	26944614

IC50	8.73		Eur. J. Med. Chem., (2016) 119:None:96	27155466

IC50	8.75		Bioorg. Med. Chem., (2014) 22:22:6438	25438768

IC50	8.79		Bioorg. Med. Chem., (2015) 23:15:4410	26169763

KIT

Tclin

Mast/stem cell growth factor receptor Kit

12 Activities

Items per page:

1 – 10 of 12

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
Kd	8.02		Nat. Biotechnol., (2011) 29:11:1046	22037378

Kd	8.12		Nat. Biotechnol., (2011) 29:11:1046	22037378

IC50	8.17		Eur. J. Med. Chem., (2014) 87:None:508	25282672

IC50	8.17		J Med Chem, (2016) 59:19:8712	27299736

IC50	8.17		Eur J Med Chem, (2016) 123:None:431	27490023

IC50	8.17		Bioorg. Med. Chem., (2015) 23:15:4410	26169763

IC50	8.4		Bioorg. Med. Chem., (2013) 21:17:5246	23838381

Kd	8.49		Nat. Biotechnol., (2011) 29:11:1046	22037378

Kd	8.57		Nat. Biotechnol., (2011) 29:11:1046	22037378

Kd	8.6		Nat. Biotechnol., (2011) 29:11:1046	22037378

FLT3

Tclin

Receptor-type tyrosine-protein kinase FLT3

12 Activities

Items per page:

1 – 10 of 12

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
Kd	7.96		Nat. Biotechnol., (2011) 29:11:1046	22037378

IC50	8.25		Eur. J. Med. Chem., (2014) 87:None:508	25282672

IC50	8.25		Bioorg. Med. Chem., (2015) 23:15:4410	26169763

IC50	8.44		J Med Chem, (2016) 59:19:8712	27299736

IC50	8.44		Eur J Med Chem, (2016) 123:None:431	27490023

Kd	8.59		Nat. Biotechnol., (2011) 29:11:1046	22037378

Kd	8.7		Nat. Biotechnol., (2011) 29:11:1046	22037378

Kd	8.82		Nat. Biotechnol., (2011) 29:11:1046	22037378

Kd	8.85		Nat. Biotechnol., (2011) 29:11:1046	22037378

Kd	9.05		Nat. Biotechnol., (2011) 29:11:1046	22037378

KDR

Tclin

Vascular endothelial growth factor receptor 2

11 Activities

Items per page:

1 – 10 of 11

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
IC50	7.8		J. Med. Chem., (2012) 55:24:10797	23098265

Kd	7.92		Nat. Biotechnol., (2011) 29:11:1046