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Assay Detail

CHEMBL830912

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

Functional
Inhibition of Hsp90 protein as degradation of HER2 kinase in SKBr3 cells
58
Total Activities
58
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type SKBr3
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Heat shock protein HSP90 (CHEMBL2095165)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Evaluation of 8-arylsulfanyl, 8-arylsulfoxyl, and 8-arylsulfonyl adenine derivatives as inhibitors of the heat shock protein 90.
Llauger L, He H, Kim J, Aguirre J, Rosen N, Peters U, Davies P, Chiosis G.
J Med Chem (2005) 48 : 2892 -2905
PubMed 15828828 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 58 4.74 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL365159 1 6.52
CHEMBL191635 1 6.09
CHEMBL193282 1 5.89
CHEMBL192145 1 5.84
CHEMBL112953 1 5.82
CHEMBL191786 1 5.66
CHEMBL273986 1 5.50
CHEMBL192062 1 5.46
CHEMBL192647 1 5.04
CHEMBL349231 1 4.98
CHEMBL192937 1 4.91
CHEMBL370247 1 4.86
CHEMBL161992 1 4.83
CHEMBL193259 1 4.68
CHEMBL190518 1 4.65
CHEMBL191268 1 4.64
CHEMBL439852 1 4.63
CHEMBL191920 1 4.58
CHEMBL364450 1 4.58
CHEMBL191241 1 4.55
CHEMBL352683 1 4.54
CHEMBL189537 1 4.50
CHEMBL364456 1 4.45
CHEMBL424824 1 4.41
CHEMBL370092 1 4.36
CHEMBL426086 1 4.35
CHEMBL194716 1 4.32
CHEMBL191601 1 4.32
CHEMBL195869 1 4.27
CHEMBL192649 1 4.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL365159 IC50 = 300.0 nM 6.52
CHEMBL191635 IC50 = 810.0 nM 6.09
CHEMBL193282 IC50 = 1300.0 nM 5.89
CHEMBL192145 IC50 = 1450.0 nM 5.84
CHEMBL112953 IC50 = 1500.0 nM 5.82
CHEMBL191786 IC50 = 2200.0 nM 5.66
CHEMBL273986 IC50 = 3200.0 nM 5.50
CHEMBL192062 IC50 = 3500.0 nM 5.46
CHEMBL192647 IC50 = 9100.0 nM 5.04
CHEMBL349231 IC50 = 10500.0 nM 4.98
CHEMBL192937 IC50 = 12400.0 nM 4.91
CHEMBL370247 IC50 = 13800.0 nM 4.86
CHEMBL161992 IC50 = 14700.0 nM 4.83
CHEMBL193259 IC50 = 20900.0 nM 4.68
CHEMBL190518 IC50 = 22300.0 nM 4.65
CHEMBL191268 IC50 = 22800.0 nM 4.64
CHEMBL439852 IC50 = 23500.0 nM 4.63
CHEMBL191920 IC50 = 26300.0 nM 4.58
CHEMBL364450 IC50 = 26500.0 nM 4.58
CHEMBL191241 IC50 = 28300.0 nM 4.55
CHEMBL352683 IC50 = 28700.0 nM 4.54
CHEMBL189537 IC50 = 31800.0 nM 4.50
CHEMBL364456 IC50 = 35900.0 nM 4.45
CHEMBL424824 IC50 = 39200.0 nM 4.41
CHEMBL370092 IC50 = 43900.0 nM 4.36
CHEMBL426086 IC50 = 44700.0 nM 4.35
CHEMBL191601 IC50 = 47600.0 nM 4.32
CHEMBL194716 IC50 = 47800.0 nM 4.32
CHEMBL195869 IC50 = 53700.0 nM 4.27
CHEMBL192649 IC50 = 57200.0 nM 4.24
CHEMBL192480 IC50 = 58000.0 nM 4.24
CHEMBL363196 IC50 = 58300.0 nM 4.23
CHEMBL192013 IC50 = 60500.0 nM 4.22
CHEMBL191668 IC50 = 65300.0 nM 4.18
CHEMBL193672 IC50 = 70300.0 nM 4.15
CHEMBL370286 IC50 = 75000.0 nM 4.12
CHEMBL191641 IC50 = 88500.0 nM 4.05
CHEMBL371372 IC50 = 97000.0 nM 4.01
CHEMBL193056 IC50 = 100000.0 nM 4.00
CHEMBL193313 IC50 > 500000.0 nM -
CHEMBL193892 IC50 > 400000.0 nM -
CHEMBL190438 IC50 > 400000.0 nM -
CHEMBL193310 IC50 = 105000.0 nM -
CHEMBL190439 IC50 = 195000.0 nM -
CHEMBL190654 IC50 = 315000.0 nM -
CHEMBL372013 IC50 = 125000.0 nM -
CHEMBL362972 IC50 = 170000.0 nM -
CHEMBL427169 IC50 = 157000.0 nM -
CHEMBL192761 IC50 = 110300.0 nM -
CHEMBL364272 IC50 = 122000.0 nM -