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Assay Detail

CHEMBL811488

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Binding
Inhibitory activity against TGF-beta type I receptor
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Thyroid hormone receptor beta (CHEMBL1947)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel and potent transforming growth factor beta type I receptor kinase domain inhibitor: 7-amino 4-(2-pyridin-2-yl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)-quinolines.
Li HY, Wang Y, Yan L, Campbell RM, Anderson BD, Wagner JR, Yingling JM.
Bioorg Med Chem Lett (2004) 14 : 3585 -3588
PubMed 15177480 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 6.44 7.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL330814 1 7.33
CHEMBL332344 1 7.32
CHEMBL121554 1 7.27
CHEMBL122583 1 7.15
CHEMBL119976 1 7.11
CHEMBL120587 1 7.06
CHEMBL121795 1 6.98
CHEMBL119936 1 6.96
CHEMBL120211 1 6.92
CHEMBL325405 1 6.82
CHEMBL121790 1 6.76
CHEMBL120718 1 6.46
CHEMBL120907 1 6.19
CHEMBL333798 1 6.06
CHEMBL120245 1 5.89
CHEMBL120799 1 5.88
CHEMBL122414 1 5.58
CHEMBL118339 1 5.40
CHEMBL331703 1 5.03
CHEMBL122524 1 4.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL330814 IC50 = 47.0 nM 7.33
CHEMBL332344 IC50 = 48.0 nM 7.32
CHEMBL121554 IC50 = 54.0 nM 7.27
CHEMBL122583 IC50 = 71.0 nM 7.15
CHEMBL119976 IC50 = 78.0 nM 7.11
CHEMBL120587 IC50 = 88.0 nM 7.06
CHEMBL121795 IC50 = 104.0 nM 6.98
CHEMBL119936 IC50 = 110.0 nM 6.96
CHEMBL120211 IC50 = 121.0 nM 6.92
CHEMBL325405 IC50 = 151.0 nM 6.82
CHEMBL121790 IC50 = 175.0 nM 6.76
CHEMBL120718 IC50 = 343.0 nM 6.46
CHEMBL120907 IC50 = 646.0 nM 6.19
CHEMBL333798 IC50 = 877.0 nM 6.06
CHEMBL120245 IC50 = 1300.0 nM 5.89
CHEMBL120799 IC50 = 1320.0 nM 5.88
CHEMBL122414 IC50 = 2620.0 nM 5.58
CHEMBL118339 IC50 = 4000.0 nM 5.40
CHEMBL331703 IC50 = 9290.0 nM 5.03
CHEMBL122524 IC50 = 19500.0 nM 4.71