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Assay Detail

CHEMBL1811085

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Binding
Inhibition of RET kinase
ChEMBL ↗
74
Total Activities
73
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Proto-oncogene tyrosine-protein kinase receptor Ret (CHEMBL2041) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Pharmacophore modeling and virtual screening to identify potential RET kinase inhibitors.
Shih KC, Shiau CW, Chen TS, Ko CH, Lin CL, Lin CY, Hwang CS, Tang CY, Chen WR, Huang JW.
Bioorg Med Chem Lett (2011) 21 : 4490 -4497
PubMed 21724393 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 74 5.85 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1807196 — — 1 8.22
CHEMBL1807197 — — 1 7.44
CHEMBL1807521 — — 1 7.42
CHEMBL248712 — — 1 7.41
CHEMBL396098 — — 1 7.30
CHEMBL1806510 — — 1 7.05
CHEMBL1807713 — — 1 6.98
CHEMBL248713 — — 2 6.97
CHEMBL1807715 — — 1 6.96
CHEMBL1807714 — — 1 6.96
CHEMBL1807716 — — 1 6.89
CHEMBL400569 — — 1 6.85
CHEMBL1807717 — — 1 6.82
CHEMBL1807198 — — 1 6.72
CHEMBL1807718 — — 1 6.70
CHEMBL1807719 — — 1 6.67
CHEMBL1807720 — — 1 6.66
CHEMBL426509 — — 1 6.47
CHEMBL1807721 — — 1 6.43
CHEMBL249502 — — 1 6.39
CHEMBL1807506 — — 1 6.39
CHEMBL1807723 — — 1 6.32
CHEMBL1807722 — — 1 6.32
CHEMBL1807507 — — 1 6.30
CHEMBL1807724 — — 1 6.27
CHEMBL1807725 — — 1 6.16
CHEMBL587723 AEE-788 2.0 1 6.13
CHEMBL1807773 — — 1 6.12
CHEMBL1807508 — — 1 6.00
CHEMBL213204 — — 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1807196 — IC50 = 6.0 nM 8.22
CHEMBL1807197 — IC50 = 36.0 nM 7.44
CHEMBL1807521 — IC50 = 38.0 nM 7.42
CHEMBL248712 — IC50 = 39.0 nM 7.41
CHEMBL396098 — IC50 = 50.0 nM 7.30
CHEMBL1806510 — IC50 = 90.0 nM 7.05
CHEMBL1807713 — IC50 = 104.0 nM 6.98
CHEMBL248713 — IC50 = 106.0 nM 6.97
CHEMBL1807715 — IC50 = 111.0 nM 6.96
CHEMBL1807714 — IC50 = 110.0 nM 6.96
CHEMBL248713 — IC50 = 110.0 nM 6.96
CHEMBL1807716 — IC50 = 128.0 nM 6.89
CHEMBL400569 — IC50 = 140.0 nM 6.85
CHEMBL1807717 — IC50 = 150.0 nM 6.82
CHEMBL1807198 — IC50 = 190.0 nM 6.72
CHEMBL1807718 — IC50 = 201.0 nM 6.70
CHEMBL1807719 — IC50 = 212.0 nM 6.67
CHEMBL1807720 — IC50 = 218.0 nM 6.66
CHEMBL426509 — IC50 = 337.0 nM 6.47
CHEMBL1807721 — IC50 = 375.0 nM 6.43
CHEMBL1807506 — IC50 = 410.0 nM 6.39
CHEMBL249502 — IC50 = 410.0 nM 6.39
CHEMBL1807723 — IC50 = 484.0 nM 6.32
CHEMBL1807722 — IC50 = 475.0 nM 6.32
CHEMBL1807507 — IC50 = 500.0 nM 6.30
CHEMBL1807724 — IC50 = 537.0 nM 6.27
CHEMBL1807725 — IC50 = 692.0 nM 6.16
CHEMBL587723 AEE-788 IC50 = 740.0 nM 6.13
CHEMBL1807773 — IC50 = 753.0 nM 6.12
CHEMBL214819 — IC50 = 1000.0 nM 6.00
CHEMBL249303 — IC50 = 1000.0 nM 6.00
CHEMBL249304 — IC50 = 1000.0 nM 6.00
CHEMBL1807774 — IC50 = 1000.0 nM 6.00
CHEMBL213204 — IC50 = 1000.0 nM 6.00
CHEMBL1807508 — IC50 = 1000.0 nM 6.00
CHEMBL249500 — IC50 = 1000.0 nM 6.00
CHEMBL220951 — IC50 = 1000.0 nM 6.00
CHEMBL1807775 — IC50 = 1073.0 nM 5.97
CHEMBL400859 — IC50 = 1100.0 nM 5.96
CHEMBL1807776 — IC50 = 1117.0 nM 5.95
CHEMBL1807777 — IC50 = 1227.0 nM 5.91
CHEMBL251739 — IC50 = 1230.0 nM 5.91
CHEMBL1807778 — IC50 = 1232.0 nM 5.91
CHEMBL1807779 — IC50 = 1262.0 nM 5.90
CHEMBL1807780 — IC50 = 1268.0 nM 5.90
CHEMBL1807509 — IC50 = 1600.0 nM 5.80
CHEMBL1807510 — IC50 = 1800.0 nM 5.75
CHEMBL1807511 — IC50 = 1800.0 nM 5.75
CHEMBL1807512 — IC50 = 2700.0 nM 5.57
CHEMBL1807781 — IC50 = 2990.0 nM 5.52