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Assay Detail

CHEMBL842210

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

Functional
Inhibitory activity against TGF-beta dependent luciferase production in mink lung cells p3TP Lux
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type lung
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 6.34 7.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL330814 1 7.66
CHEMBL120587 1 7.07
CHEMBL332344 1 7.03
CHEMBL119976 1 7.03
CHEMBL121790 1 7.02
CHEMBL122583 1 6.84
CHEMBL121554 1 6.71
CHEMBL119936 1 6.54
CHEMBL120211 1 6.52
CHEMBL121795 1 6.46
CHEMBL325405 1 6.32
CHEMBL120718 1 5.82
CHEMBL120245 1 5.70
CHEMBL333798 1 5.59
CHEMBL120799 1 5.41
CHEMBL120907 1 5.17
CHEMBL122414 1 4.93
CHEMBL331703 1 -
CHEMBL118339 1 -
CHEMBL122524 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL330814 IC50 = 22.0 nM 7.66
CHEMBL120587 IC50 = 86.0 nM 7.07
CHEMBL332344 IC50 = 93.0 nM 7.03
CHEMBL119976 IC50 = 94.0 nM 7.03
CHEMBL121790 IC50 = 96.0 nM 7.02
CHEMBL122583 IC50 = 143.0 nM 6.84
CHEMBL121554 IC50 = 196.0 nM 6.71
CHEMBL119936 IC50 = 285.0 nM 6.54
CHEMBL120211 IC50 = 304.0 nM 6.52
CHEMBL121795 IC50 = 345.0 nM 6.46
CHEMBL325405 IC50 = 475.0 nM 6.32
CHEMBL120718 IC50 = 1510.0 nM 5.82
CHEMBL120245 IC50 = 2000.0 nM 5.70
CHEMBL333798 IC50 = 2550.0 nM 5.59
CHEMBL120799 IC50 = 3860.0 nM 5.41
CHEMBL120907 IC50 = 6830.0 nM 5.17
CHEMBL122414 IC50 = 11800.0 nM 4.93
CHEMBL331703 IC50 > 20000.0 nM -
CHEMBL118339 IC50 > 20000.0 nM -
CHEMBL122524 IC50 > 20000.0 nM -