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Assay Detail

CHEMBL5515538

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

Binding
Inhibition of ALK5 signaling in mouse NIH3T3 cells transfected with (CAGA)12-luciferase reporter incubated for 18 hrs in presence of TGF-beta1 by dual-luciferase reporter assay
ChEMBL ↗
51
Total Activities
51
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type NIH3T3
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

TGF-beta receptor type-1 (CHEMBL2021750) ↗
Type SINGLE PROTEIN
Organism Mus musculus

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
EC50 51 6.53 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5557584 — — 1 7.82
CHEMBL5559089 — — 1 7.53
CHEMBL5561604 — — 1 7.34
CHEMBL5542740 — — 1 7.04
CHEMBL5558732 — — 1 6.98
CHEMBL5561520 — — 1 6.98
CHEMBL5561885 — — 1 6.89
CHEMBL5527856 — — 1 6.88
CHEMBL5566210 — — 1 6.88
CHEMBL5559812 — — 1 6.86
CHEMBL5555142 — — 1 6.75
CHEMBL5566771 — — 1 6.56
CHEMBL5558203 — — 1 6.55
CHEMBL5557295 — — 1 6.53
CHEMBL5564485 — — 1 6.52
CHEMBL5566758 — — 1 6.52
CHEMBL5559953 — — 1 6.47
CHEMBL5561312 — — 1 6.46
CHEMBL5560338 — — 1 6.44
CHEMBL5556705 — — 1 6.43
CHEMBL5568115 — — 1 6.39
CHEMBL5568195 — — 1 6.37
CHEMBL5556589 — — 1 6.36
CHEMBL5560189 — — 1 6.33
CHEMBL5563901 — — 1 6.32
CHEMBL5557476 — — 1 6.31
CHEMBL5559418 — — 1 6.28
CHEMBL5517960 — — 1 6.22
CHEMBL5566409 — — 1 6.18
CHEMBL5568200 — — 1 6.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5557584 — EC50 = 15.3 nM 7.82
CHEMBL5559089 — EC50 = 29.6 nM 7.53
CHEMBL5561604 — EC50 = 45.9 nM 7.34
CHEMBL5542740 — EC50 = 90.8 nM 7.04
CHEMBL5558732 — EC50 = 105.0 nM 6.98
CHEMBL5561520 — EC50 = 104.9 nM 6.98
CHEMBL5561885 — EC50 = 129.7 nM 6.89
CHEMBL5527856 — EC50 = 131.2 nM 6.88
CHEMBL5566210 — EC50 = 132.4 nM 6.88
CHEMBL5559812 — EC50 = 137.9 nM 6.86
CHEMBL5555142 — EC50 = 175.9 nM 6.75
CHEMBL5566771 — EC50 = 273.2 nM 6.56
CHEMBL5558203 — EC50 = 283.5 nM 6.55
CHEMBL5557295 — EC50 = 294.7 nM 6.53
CHEMBL5566758 — EC50 = 302.6 nM 6.52
CHEMBL5564485 — EC50 = 302.2 nM 6.52
CHEMBL5559953 — EC50 = 338.6 nM 6.47
CHEMBL5561312 — EC50 = 348.4 nM 6.46
CHEMBL5560338 — EC50 = 362.6 nM 6.44
CHEMBL5556705 — EC50 = 373.6 nM 6.43
CHEMBL5568115 — EC50 = 403.4 nM 6.39
CHEMBL5568195 — EC50 = 429.7 nM 6.37
CHEMBL5556589 — EC50 = 441.2 nM 6.36
CHEMBL5560189 — EC50 = 464.8 nM 6.33
CHEMBL5563901 — EC50 = 484.7 nM 6.32
CHEMBL5557476 — EC50 = 487.6 nM 6.31
CHEMBL5559418 — EC50 = 525.3 nM 6.28
CHEMBL5517960 — EC50 = 606.6 nM 6.22
CHEMBL5566409 — EC50 = 664.8 nM 6.18
CHEMBL5568200 — EC50 = 682.2 nM 6.17
CHEMBL5555707 — EC50 = 688.8 nM 6.16
CHEMBL5568196 — EC50 = 749.8 nM 6.12
CHEMBL5561489 — EC50 = 848.0 nM 6.07
CHEMBL5568406 — EC50 = 855.8 nM 6.07
CHEMBL5560056 — EC50 = 970.6 nM 6.01
CHEMBL5562142 — EC50 = 998.4 nM 6.00
CHEMBL5566711 — EC50 = 1325.0 nM 5.88
CHEMBL5565272 — EC50 > 1000.0 nM -
CHEMBL5557497 — EC50 > 1000.0 nM -
CHEMBL5559936 — EC50 > 1000.0 nM -
CHEMBL5523453 — EC50 > 1000.0 nM -
CHEMBL5556297 — EC50 > 1000.0 nM -
CHEMBL5557910 — EC50 > 1000.0 nM -
CHEMBL5557039 — EC50 > 1000.0 nM -
CHEMBL5532038 — EC50 > 1000.0 nM -
CHEMBL5559086 — EC50 > 1000.0 nM -
CHEMBL5568184 — EC50 > 1000.0 nM -
CHEMBL5557837 — EC50 > 1000.0 nM -
CHEMBL5555841 — EC50 > 1000.0 nM -
CHEMBL5523459 — EC50 > 1000.0 nM -