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Assay Detail

CHEMBL828472

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

Binding
Inhibitory concentration exhibited towards MSK-1
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Ribosomal protein S6 kinase alpha-5 (CHEMBL4237)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

(1H-imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: a novel class of potent MSK-1-inhibitors.
Bamford MJ, Alberti MJ, Bailey N, Davies S, Dean DK, Gaiba A, Garland S, Harling JD, Jung DK, Panchal TA, Parr CA, Steadman JG, Takle AK, Townsend JT, Wilson DM, Witherington J.
Bioorg Med Chem Lett (2005) 15 : 3402 -3406
PubMed 15950465 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 6.93 8.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL185962 1 8.74
CHEMBL189231 1 8.52
CHEMBL189657 1 8.52
CHEMBL188433 1 7.96
CHEMBL188457 1 7.89
CHEMBL363054 1 7.77
CHEMBL189094 1 7.77
CHEMBL189299 1 7.70
CHEMBL187339 1 7.42
CHEMBL361678 1 7.26
CHEMBL191104 1 6.97
CHEMBL188048 1 6.90
CHEMBL365286 GW549034X 1 6.85
CHEMBL365902 1 6.59
CHEMBL185731 1 6.01
CHEMBL362712 1 5.92
CHEMBL189120 1 5.82
CHEMBL185710 1 5.81
CHEMBL361690 1 5.71
CHEMBL426800 GW785404X 1 5.67
CHEMBL364990 1 5.36
CHEMBL362494 1 5.29
CHEMBL188342 1 -
CHEMBL363546 1 -
CHEMBL188543 1 -
CHEMBL188571 1 -
CHEMBL188908 1 -
CHEMBL372432 1 -
CHEMBL361257 1 -
CHEMBL185689 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL185962 IC50 = 1.8 nM 8.74
CHEMBL189231 IC50 = 3.0 nM 8.52
CHEMBL189657 IC50 = 3.0 nM 8.52
CHEMBL188433 IC50 = 11.0 nM 7.96
CHEMBL188457 IC50 = 13.0 nM 7.89
CHEMBL363054 IC50 = 17.0 nM 7.77
CHEMBL189094 IC50 = 17.0 nM 7.77
CHEMBL189299 IC50 = 20.0 nM 7.70
CHEMBL187339 IC50 = 38.0 nM 7.42
CHEMBL361678 IC50 = 55.0 nM 7.26
CHEMBL191104 IC50 = 107.0 nM 6.97
CHEMBL188048 IC50 = 126.0 nM 6.90
CHEMBL365286 GW549034X IC50 = 140.0 nM 6.85
CHEMBL365902 IC50 = 258.0 nM 6.59
CHEMBL185731 IC50 = 974.0 nM 6.01
CHEMBL362712 IC50 = 1200.0 nM 5.92
CHEMBL189120 IC50 = 1520.0 nM 5.82
CHEMBL185710 IC50 = 1540.0 nM 5.81
CHEMBL361690 IC50 = 1960.0 nM 5.71
CHEMBL426800 GW785404X IC50 = 2120.0 nM 5.67
CHEMBL364990 IC50 = 4390.0 nM 5.36
CHEMBL362494 IC50 = 5097.0 nM 5.29
CHEMBL188342 IC50 > 10000.0 nM -
CHEMBL363546 IC50 > 10000.0 nM -
CHEMBL188543 IC50 > 10000.0 nM -
CHEMBL188571 IC50 > 10000.0 nM -
CHEMBL188908 IC50 > 10000.0 nM -
CHEMBL372432 IC50 > 10000.0 nM -
CHEMBL361257 IC50 > 10000.0 nM -
CHEMBL185689 IC50 > 10000.0 nM -
CHEMBL415769 IC50 > 10000.0 nM -