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Assay Detail

CHEMBL1838880

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

Binding
Binding affinity to human HSP90alpha assessed as 2D1H-15N chemical shift perturbation by NMR spectroscopy
23
Total Activities
23
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 HSP 90-alpha (CHEMBL3880)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Lead generation of heat shock protein 90 inhibitors by a combination of fragment-based approach, virtual screening, and structure-based drug design.
Miura T, Fukami TA, Hasegawa K, Ono N, Suda A, Shindo H, Yoon DO, Kim SJ, Na YJ, Aoki Y, Shimma N, Tsukuda T, Shiratori Y.
Bioorg Med Chem Lett (2011) 21 : 5778 -5783
PubMed 21875802 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 23 5.76 8.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1834096 1 8.47
CHEMBL1834390 1 7.38
CHEMBL109480 TANESPIMYCIN 3.0 1 6.66
CHEMBL1834093 1 6.64
CHEMBL1834385 1 6.54
CHEMBL1834386 1 6.48
CHEMBL1834387 1 6.47
CHEMBL1834388 1 6.24
CHEMBL1834091 1 6.07
CHEMBL313528 1 5.64
CHEMBL1834090 1 5.43
CHEMBL1834094 1 5.35
CHEMBL86795 INDAZOLE 1 5.28
CHEMBL1834095 1 5.16
CHEMBL89436 1 5.00
CHEMBL88580 1 4.72
CHEMBL561426 1 4.29
CHEMBL1834089 1 4.10
CHEMBL302453 1 3.52
CHEMBL1834088 1 -
CHEMBL1834092 1 -
CHEMBL1834389 1 -
CHEMBL21619 2-AMINOPYRIDINE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1834096 Kd = 3.4 nM 8.47
CHEMBL1834390 Kd = 42.0 nM 7.38
CHEMBL109480 TANESPIMYCIN Kd = 220.0 nM 6.66
CHEMBL1834093 Kd = 230.0 nM 6.64
CHEMBL1834385 Kd = 290.0 nM 6.54
CHEMBL1834386 Kd = 330.0 nM 6.48
CHEMBL1834387 Kd = 340.0 nM 6.47
CHEMBL1834388 Kd = 570.0 nM 6.24
CHEMBL1834091 Kd = 860.0 nM 6.07
CHEMBL313528 Kd = 2300.0 nM 5.64
CHEMBL1834090 Kd = 3700.0 nM 5.43
CHEMBL1834094 Kd = 4500.0 nM 5.35
CHEMBL86795 INDAZOLE Kd = 5300.0 nM 5.28
CHEMBL1834095 Kd = 6900.0 nM 5.16
CHEMBL89436 Kd = 10000.0 nM 5.00
CHEMBL88580 Kd = 19000.0 nM 4.72
CHEMBL561426 Kd = 51000.0 nM 4.29
CHEMBL1834089 Kd = 79000.0 nM 4.10
CHEMBL302453 Kd = 300000.0 nM 3.52
CHEMBL1834088 Kd > 1000.0 nM -
CHEMBL1834092 Kd - -
CHEMBL1834389 Kd > 1000.0 nM -
CHEMBL21619 2-AMINOPYRIDINE Kd > 1000.0 nM -