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Assay Detail

CHEMBL5526754

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

Binding
Inhibition of N-terminal 6xHis tagged human Hsp70 expressed in Escherichia coli BL21 (DE3)/FAM-labeled BimBH3 peptide (unknown origin) protein protein interaction incubated for 10 mins by fluorescence polarization assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of Biphenyl Derivatives to Target Hsp70-Bim Protein-Protein Interaction in Chronic Myeloid Leukemia by Scaffold Hopping Strategy.
Jiang M, Zhang H, Song Y, Yin F, Hu Z, Li X, Wang Y, Wang Z, Li Y, Wang Z, Zhang Y, Wang S, Lu S, Xu G, Song T, Wang Z, Zhang Z.
J Med Chem (2024) 67 : 12068 -12084
PubMed 39012838 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 6.10 7.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5555840 1 7.16
CHEMBL5564252 1 7.05
CHEMBL5559278 1 6.55
CHEMBL5564322 1 6.48
CHEMBL5559963 1 6.39
CHEMBL5562172 1 6.21
CHEMBL5397919 1 6.10
CHEMBL5565321 1 6.09
CHEMBL5563022 1 6.06
CHEMBL5561641 1 6.03
CHEMBL5562439 1 5.67
CHEMBL5565355 1 5.44
CHEMBL5561415 1 5.09
CHEMBL5542768 1 5.06
CHEMBL5562006 1 -
CHEMBL5568002 1 -
CHEMBL5560223 1 -
CHEMBL5567472 1 -
CHEMBL5565964 1 -
CHEMBL5565577 1 -
CHEMBL5555383 1 -
CHEMBL5563334 1 -
CHEMBL5542337 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5555840 IC50 = 70.0 nM 7.16
CHEMBL5564252 IC50 = 90.0 nM 7.05
CHEMBL5559278 IC50 = 280.0 nM 6.55
CHEMBL5564322 IC50 = 330.0 nM 6.48
CHEMBL5559963 IC50 = 410.0 nM 6.39
CHEMBL5562172 IC50 = 620.0 nM 6.21
CHEMBL5397919 IC50 = 800.0 nM 6.10
CHEMBL5565321 IC50 = 820.0 nM 6.09
CHEMBL5563022 IC50 = 880.0 nM 6.06
CHEMBL5561641 IC50 = 930.0 nM 6.03
CHEMBL5562439 IC50 = 2130.0 nM 5.67
CHEMBL5565355 IC50 = 3600.0 nM 5.44
CHEMBL5561415 IC50 = 8200.0 nM 5.09
CHEMBL5542768 IC50 = 8800.0 nM 5.06
CHEMBL5562006 IC50 > 10000.0 nM -
CHEMBL5568002 IC50 > 10000.0 nM -
CHEMBL5560223 IC50 > 10000.0 nM -
CHEMBL5567472 IC50 > 10000.0 nM -
CHEMBL5565964 IC50 > 10000.0 nM -
CHEMBL5565577 IC50 > 10000.0 nM -
CHEMBL5555383 IC50 > 10000.0 nM -
CHEMBL5563334 IC50 > 10000.0 nM -
CHEMBL5542337 IC50 > 10000.0 nM -