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Assay Detail

CHEMBL3418289

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of recombinant c-Met kinase domain (unknown origin) incubated for 30 mins using gastrin peptide substrate by HTRF assay
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Hepatocyte growth factor receptor (CHEMBL3717)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of potent and selective 8-fluorotriazolopyridine c-Met inhibitors.
Peterson EA, Teffera Y, Albrecht BK, Bauer D, Bellon SF, Boezio A, Boezio C, Broome MA, Choquette D, Copeland KW, Dussault I, Lewis R, Lin MH, Lohman J, Liu J, Potashman M, Rex K, Shimanovich R, Whittington DA, Vaida KR, Harmange JC.
J Med Chem (2015) 58 : 2417 -2430
PubMed 25699405 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 37 7.78 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3414922 1 9.00
CHEMBL3414926 1 9.00
CHEMBL3414925 1 8.70
CHEMBL3414923 1 8.70
CHEMBL3414918 1 8.70
CHEMBL3414914 1 8.70
CHEMBL3414913 1 8.52
CHEMBL3414738 1 8.40
CHEMBL3414919 1 8.30
CHEMBL3414917 1 8.30
CHEMBL3414577 1 8.30
CHEMBL3414731 1 8.15
CHEMBL3414920 1 8.15
CHEMBL3414921 1 8.05
CHEMBL3414736 1 8.05
CHEMBL496102 AMG-208 2.0 1 8.05
CHEMBL3414742 1 7.96
CHEMBL3414737 1 7.96
CHEMBL3414915 1 7.92
CHEMBL3414735 1 7.92
CHEMBL3414741 1 7.75
CHEMBL3414739 1 7.66
CHEMBL3414734 1 7.64
CHEMBL3414740 1 7.62
CHEMBL3414929 1 7.55
CHEMBL3414730 1 7.51
CHEMBL3414743 1 7.29
CHEMBL3414912 1 7.28
CHEMBL3414733 1 7.22
CHEMBL3414745 1 7.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3414922 IC50 = 1.0 nM 9.00
CHEMBL3414926 IC50 = 1.0 nM 9.00
CHEMBL3414923 IC50 = 2.0 nM 8.70
CHEMBL3414918 IC50 = 2.0 nM 8.70
CHEMBL3414914 IC50 = 2.0 nM 8.70
CHEMBL3414925 IC50 = 2.0 nM 8.70
CHEMBL3414913 IC50 = 3.0 nM 8.52
CHEMBL3414738 IC50 = 4.0 nM 8.40
CHEMBL3414577 IC50 = 5.0 nM 8.30
CHEMBL3414917 IC50 = 5.0 nM 8.30
CHEMBL3414919 IC50 = 5.0 nM 8.30
CHEMBL3414731 IC50 = 7.0 nM 8.15
CHEMBL3414920 IC50 = 7.0 nM 8.15
CHEMBL496102 AMG-208 IC50 = 9.0 nM 8.05
CHEMBL3414736 IC50 = 9.0 nM 8.05
CHEMBL3414921 IC50 = 9.0 nM 8.05
CHEMBL3414742 IC50 = 11.0 nM 7.96
CHEMBL3414737 IC50 = 11.0 nM 7.96
CHEMBL3414915 IC50 = 12.0 nM 7.92
CHEMBL3414735 IC50 = 12.0 nM 7.92
CHEMBL3414741 IC50 = 18.0 nM 7.75
CHEMBL3414739 IC50 = 22.0 nM 7.66
CHEMBL3414734 IC50 = 23.0 nM 7.64
CHEMBL3414740 IC50 = 24.0 nM 7.62
CHEMBL3414929 IC50 = 28.0 nM 7.55
CHEMBL3414730 IC50 = 31.0 nM 7.51
CHEMBL3414743 IC50 = 51.0 nM 7.29
CHEMBL3414912 IC50 = 52.0 nM 7.28
CHEMBL3414733 IC50 = 60.0 nM 7.22
CHEMBL3414745 IC50 = 67.0 nM 7.17
CHEMBL3414928 IC50 = 93.0 nM 7.03
CHEMBL3414744 IC50 = 182.0 nM 6.74
CHEMBL3414732 IC50 = 210.0 nM 6.68
CHEMBL3414924 IC50 = 370.0 nM 6.43
CHEMBL3414916 IC50 = 780.0 nM 6.11
CHEMBL496101 IC50 = 2100.0 nM 5.68
CHEMBL3414927 IC50 > 400.0 nM -