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Assay Detail

CHEMBL4823577

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

Binding
Inhibition of AXL (unknown origin) using poly [Glu, Tyr] 4:1 as substrate incubated for 60 mins in presence of ATP by ELISA
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

Tyrosine-protein kinase receptor UFO (CHEMBL4895)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a Pyrimidinedione Derivative as a Potent and Orally Bioavailable Axl Inhibitor.
Zhang H, Peng X, Dai Y, Shao J, Ji Y, Sun Y, Liu B, Cheng X, Ai J, Duan W.
J Med Chem (2021) 64 : 3956 -3975
PubMed 33733758 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 37 7.90 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4871310 1 9.10
CHEMBL4873571 1 9.05
CHEMBL4861161 1 8.77
CHEMBL4858048 1 8.72
CHEMBL4863290 1 8.56
CHEMBL4869458 1 8.51
CHEMBL4864676 1 8.43
CHEMBL3301622 GILTERITINIB 4.0 1 8.34
CHEMBL3809489 BEMCENTINIB 2.0 1 8.32
CHEMBL4846125 1 8.31
CHEMBL4867669 1 8.26
CHEMBL4855681 1 8.24
CHEMBL4856526 1 8.17
CHEMBL4856234 1 8.10
CHEMBL4875798 1 8.07
CHEMBL4851321 1 8.06
CHEMBL4875876 1 8.06
CHEMBL4846678 1 7.98
CHEMBL4856142 1 7.89
CHEMBL4853182 1 7.78
CHEMBL4848473 1 7.76
CHEMBL4861226 1 7.69
CHEMBL4864426 1 7.66
CHEMBL4863687 1 7.59
CHEMBL4872759 1 7.58
CHEMBL4849593 1 7.34
CHEMBL4858649 1 7.23
CHEMBL4866212 1 6.82
CHEMBL4856528 1 6.75
CHEMBL4856829 1 6.73

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4871310 IC50 = 0.8 nM 9.10
CHEMBL4873571 IC50 = 0.9 nM 9.05
CHEMBL4861161 IC50 = 1.7 nM 8.77
CHEMBL4858048 IC50 = 1.9 nM 8.72
CHEMBL4863290 IC50 = 2.75 nM 8.56
CHEMBL4869458 IC50 = 3.1 nM 8.51
CHEMBL4864676 IC50 = 3.7 nM 8.43
CHEMBL3301622 GILTERITINIB IC50 = 4.6 nM 8.34
CHEMBL3809489 BEMCENTINIB IC50 = 4.8 nM 8.32
CHEMBL4846125 IC50 = 4.9 nM 8.31
CHEMBL4867669 IC50 = 5.5 nM 8.26
CHEMBL4855681 IC50 = 5.8 nM 8.24
CHEMBL4856526 IC50 = 6.7 nM 8.17
CHEMBL4856234 IC50 = 8.0 nM 8.10
CHEMBL4875798 IC50 = 8.6 nM 8.07
CHEMBL4851321 IC50 = 8.8 nM 8.06
CHEMBL4875876 IC50 = 8.7 nM 8.06
CHEMBL4846678 IC50 = 10.5 nM 7.98
CHEMBL4856142 IC50 = 13.0 nM 7.89
CHEMBL4853182 IC50 = 16.8 nM 7.78
CHEMBL4848473 IC50 = 17.4 nM 7.76
CHEMBL4861226 IC50 = 20.5 nM 7.69
CHEMBL4864426 IC50 = 21.9 nM 7.66
CHEMBL4863687 IC50 = 25.6 nM 7.59
CHEMBL4872759 IC50 = 26.0 nM 7.58
CHEMBL4849593 IC50 = 45.6 nM 7.34
CHEMBL4858649 IC50 = 58.3 nM 7.23
CHEMBL4866212 IC50 = 150.0 nM 6.82
CHEMBL4856528 IC50 = 178.6 nM 6.75
CHEMBL4856829 IC50 = 184.8 nM 6.73
CHEMBL4845715 IC50 = 253.9 nM 6.59
CHEMBL4879206 IC50 = 395.7 nM 6.40
CHEMBL4863885 IC50 > 1000.0 nM -
CHEMBL4848206 IC50 > 1000.0 nM -
CHEMBL4864950 IC50 > 1000.0 nM -
CHEMBL4862247 IC50 > 1000.0 nM -
CHEMBL4848709 IC50 > 1000.0 nM -