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Assay Detail

CHEMBL4769705

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

Binding
Inhibition of ALK5 (unknown origin) measured after 120 mins of incubation by ADP-Glo kinase assay
28
Total Activities
28
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

TGF-beta receptor type-1 (CHEMBL4439)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological evaluation of 4-(pyridin-4-oxy)-3-(3,3-difluorocyclobutyl)-pyrazole derivatives as novel potent transforming growth factor-β type 1 receptor inhibitors.
Xu G,Zhang Y,Wang H,Guo Z,Wang X,Li X,Chang S,Sun T,Yu Z,Xu T,Zhao L,Wang Y,Yu W
Eur J Med Chem (2020) 198 : 112354 -112354
PubMed 32387837 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 7.27 8.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4782867 1 8.09
CHEMBL4797447 1 8.09
CHEMBL4791582 1 7.94
CHEMBL4777294 1 7.88
CHEMBL4788502 1 7.88
CHEMBL4792452 1 7.71
CHEMBL4784194 1 7.66
CHEMBL4780548 1 7.61
CHEMBL4777871 1 7.58
CHEMBL4786439 1 7.58
CHEMBL4797329 1 7.56
CHEMBL4781586 1 7.52
CHEMBL4790322 1 7.50
CHEMBL4791955 1 7.50
CHEMBL4778362 1 7.46
CHEMBL4594432 LY-3200882 1.0 1 7.42
CHEMBL4791815 1 7.36
CHEMBL4788673 1 7.36
CHEMBL4795823 1 7.33
CHEMBL4784622 1 7.21
CHEMBL4781326 1 7.16
CHEMBL4777610 1 7.08
CHEMBL4781452 1 6.55
CHEMBL4799736 1 6.51
CHEMBL4795745 1 6.38
CHEMBL4783147 1 6.28
CHEMBL4794175 1 6.09
CHEMBL4784607 1 5.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4782867 IC50 = 8.2 nM 8.09
CHEMBL4797447 IC50 = 8.2 nM 8.09
CHEMBL4791582 IC50 = 11.4 nM 7.94
CHEMBL4777294 IC50 = 13.2 nM 7.88
CHEMBL4788502 IC50 = 13.2 nM 7.88
CHEMBL4792452 IC50 = 19.7 nM 7.71
CHEMBL4784194 IC50 = 21.7 nM 7.66
CHEMBL4780548 IC50 = 24.3 nM 7.61
CHEMBL4777871 IC50 = 26.2 nM 7.58
CHEMBL4786439 IC50 = 26.0 nM 7.58
CHEMBL4797329 IC50 = 27.5 nM 7.56
CHEMBL4781586 IC50 = 30.2 nM 7.52
CHEMBL4790322 IC50 = 31.4 nM 7.50
CHEMBL4791955 IC50 = 31.4 nM 7.50
CHEMBL4778362 IC50 = 34.6 nM 7.46
CHEMBL4594432 LY-3200882 IC50 = 38.2 nM 7.42
CHEMBL4791815 IC50 = 44.0 nM 7.36
CHEMBL4788673 IC50 = 44.2 nM 7.36
CHEMBL4795823 IC50 = 47.2 nM 7.33
CHEMBL4784622 IC50 = 61.3 nM 7.21
CHEMBL4781326 IC50 = 69.2 nM 7.16
CHEMBL4777610 IC50 = 84.0 nM 7.08
CHEMBL4781452 IC50 = 282.0 nM 6.55
CHEMBL4799736 IC50 = 308.0 nM 6.51
CHEMBL4795745 IC50 = 416.0 nM 6.38
CHEMBL4783147 IC50 = 528.0 nM 6.28
CHEMBL4794175 IC50 = 814.0 nM 6.09
CHEMBL4784607 IC50 = 6736.0 nM 5.17