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Assay Detail

CHEMBL5515537

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

Binding
Inhibition of ALK5 (unknown origin) incubated for 2 hrs in presence of ATP by ADP-Glo reagent based luminescence plate reader analysis
22
Total Activities
22
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

Design, synthesis and evaluation of a pyrazolo[3,4-d]pyrimidine derivative as a novel and potent TGFβ1R1 inhibitor.
Wang Y, Liu Y, Zhang Y, Zhang Z, Xu L, Wang J, Yang Y, Hu B, Yao Y, Wei M, Wang J, Tang B, Zhang K, Liu S, Yang G.
Eur J Med Chem (2024) 271 : 116395 -116395
PubMed 38626523 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.76 7.76

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5557584 1 7.76
CHEMBL5559089 1 7.32
CHEMBL2364611 GALUNISERTIB 2.0 1 7.30
CHEMBL5527856 1 7.19
CHEMBL5555142 1 7.17
CHEMBL5561604 1 7.10
CHEMBL5561885 1 7.04
CHEMBL5566771 1 6.88
CHEMBL5558203 1 6.86
CHEMBL5560338 1 6.81
CHEMBL5559812 1 6.75
CHEMBL5561312 1 6.74
CHEMBL5561520 1 6.58
CHEMBL5566758 1 6.57
CHEMBL5568115 1 6.56
CHEMBL5557295 1 6.51
CHEMBL5564485 1 6.41
CHEMBL5542740 1 6.39
CHEMBL5556705 1 6.28
CHEMBL5558732 1 6.22
CHEMBL5566210 1 6.19
CHEMBL5559953 1 6.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5557584 IC50 = 17.3 nM 7.76
CHEMBL5559089 IC50 = 48.3 nM 7.32
CHEMBL2364611 GALUNISERTIB IC50 = 50.1 nM 7.30
CHEMBL5527856 IC50 = 64.7 nM 7.19
CHEMBL5555142 IC50 = 67.8 nM 7.17
CHEMBL5561604 IC50 = 80.2 nM 7.10
CHEMBL5561885 IC50 = 91.3 nM 7.04
CHEMBL5566771 IC50 = 132.6 nM 6.88
CHEMBL5558203 IC50 = 137.9 nM 6.86
CHEMBL5560338 IC50 = 155.1 nM 6.81
CHEMBL5559812 IC50 = 176.3 nM 6.75
CHEMBL5561312 IC50 = 181.8 nM 6.74
CHEMBL5561520 IC50 = 262.3 nM 6.58
CHEMBL5566758 IC50 = 270.5 nM 6.57
CHEMBL5568115 IC50 = 273.5 nM 6.56
CHEMBL5557295 IC50 = 309.0 nM 6.51
CHEMBL5564485 IC50 = 386.4 nM 6.41
CHEMBL5542740 IC50 = 407.9 nM 6.39
CHEMBL5556705 IC50 = 521.3 nM 6.28
CHEMBL5558732 IC50 = 596.7 nM 6.22
CHEMBL5566210 IC50 = 649.0 nM 6.19
CHEMBL5559953 IC50 = 873.5 nM 6.06