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Assay Detail

CHEMBL4001302

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

Binding
Inhibition of bisamide probe binding to pirin in human SKOV3 cells by SILAC-based quantitative mass spectrometry pull down assay
4
Total Activities
2
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Pirin (CHEMBL2010627)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a Chemical Probe Bisamide (CCT251236): An Orally Bioavailable Efficacious Pirin Ligand from a Heat Shock Transcription Factor 1 (HSF1) Phenotypic Screen.
Cheeseman MD, Chessum NE, Rye CS, Pasqua AE, Tucker MJ, Wilding B, Evans LE, Lepri S, Richards M, Sharp SY, Ali S, Rowlands M, O'Fee L, Miah A, Hayes A, Henley AT, Powers M, Te Poele R, De Billy E, Pellegrino L, Raynaud F, Burke R, van Montfort RL, Eccles SA, Workman P, Jones K.
J Med Chem (2017) 60 : 180 -201
PubMed 28004573 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
AC50 2 5.41 5.82
Ki 2 7.14 7.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4087666 2 7.55
CHEMBL4096048 2 6.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4087666 Ki = 28.0 nM 7.55
CHEMBL4096048 Ki = 190.0 nM 6.72
CHEMBL4087666 AC50 = 1500.0 nM 5.82
CHEMBL4096048 AC50 = 10000.0 nM 5.00