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Assay Detail

CHEMBL1103914

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

Binding
Inhibition of TPR-tagged RON catalytic domain expressed in HEK293 cells
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HEK293
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Macrophage-stimulating protein receptor (CHEMBL2689)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of a novel series of potent RON receptor tyrosine kinase inhibitors.
Raeppel S, Gaudette F, Mannion M, Claridge S, Saavedra O, Isakovic L, Déziel R, Beaulieu N, Beaulieu C, Dupont I, Nguyen H, Wang J, Macleod AR, Maroun C, Besterman JM, Vaisburg A.
Bioorg Med Chem Lett (2010) 20 : 2745 -2749
PubMed 20363625 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 6.95 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1095359 1 7.52
CHEMBL1095356 1 7.52
CHEMBL1095360 1 7.40
CHEMBL1094718 1 7.30
CHEMBL1095035 1 7.22
CHEMBL1095034 1 7.22
CHEMBL1087984 1 7.10
CHEMBL1095036 1 7.10
CHEMBL1095357 1 7.05
CHEMBL1095361 1 7.05
CHEMBL1095358 1 7.00
CHEMBL1086932 1 6.82
CHEMBL462232 1 6.77
CHEMBL1098158 1 6.70
CHEMBL1086675 1 6.68
CHEMBL600632 1 6.39
CHEMBL1086676 1 6.23
CHEMBL602703 1 5.99
CHEMBL1098157 1 -
CHEMBL1097824 1 -
CHEMBL1088539 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1095359 IC50 = 30.0 nM 7.52
CHEMBL1095356 IC50 = 30.0 nM 7.52
CHEMBL1095360 IC50 = 40.0 nM 7.40
CHEMBL1094718 IC50 = 50.0 nM 7.30
CHEMBL1095035 IC50 = 60.0 nM 7.22
CHEMBL1095034 IC50 = 60.0 nM 7.22
CHEMBL1087984 IC50 = 80.0 nM 7.10
CHEMBL1095036 IC50 = 80.0 nM 7.10
CHEMBL1095357 IC50 = 90.0 nM 7.05
CHEMBL1095361 IC50 = 90.0 nM 7.05
CHEMBL1095358 IC50 = 100.0 nM 7.00
CHEMBL1086932 IC50 = 150.0 nM 6.82
CHEMBL462232 IC50 = 170.0 nM 6.77
CHEMBL1098158 IC50 = 200.0 nM 6.70
CHEMBL1086675 IC50 = 210.0 nM 6.68
CHEMBL600632 IC50 = 410.0 nM 6.39
CHEMBL1086676 IC50 = 590.0 nM 6.23
CHEMBL602703 IC50 = 1030.0 nM 5.99
CHEMBL1098157 IC50 > 1000.0 nM -
CHEMBL1097824 IC50 > 1000.0 nM -
CHEMBL1088539 IC50 > 10000.0 nM -