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Assay Detail

CHEMBL5625560

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Binding
Binding affinity to TRAP1 (unknown origin) assessed as dissociation constant incubated for 24 hrs by fluorescence polarization 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

Heat shock protein 75 kDa, mitochondrial (CHEMBL1075132)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Elucidation of novel TRAP1-Selective inhibitors that regulate mitochondrial processes.
Merfeld T, Peng S, Keegan BM, Crowley VM, Brackett CM, Gutierrez A, McCann NR, Reynolds TS, Rhodes MC, Byrd KM, Deng J, Matts RL, Blagg BSJ.
Eur J Med Chem (2023) 258 : 115531 -115531
PubMed 37307624 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 28 6.38 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5633903 1 7.40
CHEMBL5633816 1 7.40
CHEMBL5633571 1 7.10
CHEMBL5633012 1 7.05
CHEMBL5632075 1 7.05
CHEMBL5631806 1 6.80
CHEMBL5633174 1 6.64
CHEMBL200102 PU-H71 2.0 1 6.62
CHEMBL5631336 1 6.46
CHEMBL5633431 1 6.44
CHEMBL5633987 1 6.42
CHEMBL3260480 1 6.38
CHEMBL5631777 1 6.38
CHEMBL5632244 1 6.33
CHEMBL5633752 1 6.33
CHEMBL5631620 1 6.31
CHEMBL5631997 1 6.26
CHEMBL5631343 1 6.19
CHEMBL5631613 1 6.07
CHEMBL5632194 1 6.05
CHEMBL5631423 1 6.03
CHEMBL5631707 1 6.02
CHEMBL5629930 1 5.61
CHEMBL5633082 1 5.60
CHEMBL5631756 1 5.58
CHEMBL5633971 1 5.39
CHEMBL5633893 1 -
CHEMBL5632487 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5633903 Kd = 40.0 nM 7.40
CHEMBL5633816 Kd = 40.0 nM 7.40
CHEMBL5633571 Kd = 80.0 nM 7.10
CHEMBL5633012 Kd = 90.0 nM 7.05
CHEMBL5632075 Kd = 90.0 nM 7.05
CHEMBL5631806 Kd = 160.0 nM 6.80
CHEMBL5633174 Kd = 230.0 nM 6.64
CHEMBL200102 PU-H71 Kd = 240.0 nM 6.62
CHEMBL5631336 Kd = 350.0 nM 6.46
CHEMBL5633431 Kd = 360.0 nM 6.44
CHEMBL5633987 Kd = 380.0 nM 6.42
CHEMBL3260480 Kd = 420.0 nM 6.38
CHEMBL5631777 Kd = 420.0 nM 6.38
CHEMBL5632244 Kd = 470.0 nM 6.33
CHEMBL5633752 Kd = 470.0 nM 6.33
CHEMBL5631620 Kd = 490.0 nM 6.31
CHEMBL5631997 Kd = 550.0 nM 6.26
CHEMBL5631343 Kd = 650.0 nM 6.19
CHEMBL5631613 Kd = 860.0 nM 6.07
CHEMBL5632194 Kd = 890.0 nM 6.05
CHEMBL5631423 Kd = 930.0 nM 6.03
CHEMBL5631707 Kd = 960.0 nM 6.02
CHEMBL5629930 Kd = 2430.0 nM 5.61
CHEMBL5633082 Kd = 2500.0 nM 5.60
CHEMBL5631756 Kd = 2630.0 nM 5.58
CHEMBL5633971 Kd = 4040.0 nM 5.39
CHEMBL5633893 Kd > 5000.0 nM -
CHEMBL5632487 Kd > 100000.0 nM -