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Assay Detail

CHEMBL877123

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Binding
Inhibitory concentration against MSK-1
25
Total Activities
25
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: further optimisation as highly potent and selective MSK-1-inhibitors.
Bamford MJ, Bailey N, Davies S, Dean DK, Francis L, Panchal TA, Parr CA, Sehmi S, Steadman JG, Takle AK, Townsend JT, Wilson DM.
Bioorg Med Chem Lett (2005) 15 : 3407 -3411
PubMed 15955699 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 7.74 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL188434 1 9.30
CHEMBL415770 1 8.85
CHEMBL185962 1 8.82
CHEMBL188806 1 8.70
CHEMBL186317 1 8.60
CHEMBL189657 1 8.52
CHEMBL426440 1 8.52
CHEMBL189231 1 8.52
CHEMBL187340 1 8.40
CHEMBL188268 1 8.40
CHEMBL188433 1 8.22
CHEMBL360219 1 8.15
CHEMBL364413 1 8.10
CHEMBL188620 1 8.05
CHEMBL365832 1 8.05
CHEMBL363258 1 7.89
CHEMBL363054 1 7.77
CHEMBL189773 1 7.66
CHEMBL188240 1 6.76
CHEMBL363990 1 6.68
CHEMBL365072 1 6.64
CHEMBL191105 1 6.21
CHEMBL186343 1 6.09
CHEMBL187985 1 5.65
CHEMBL371391 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL188434 IC50 = 0.5 nM 9.30
CHEMBL415770 IC50 = 1.4 nM 8.85
CHEMBL185962 IC50 = 1.5 nM 8.82
CHEMBL188806 IC50 = 2.0 nM 8.70
CHEMBL186317 IC50 = 2.5 nM 8.60
CHEMBL189657 IC50 = 3.0 nM 8.52
CHEMBL426440 IC50 = 3.0 nM 8.52
CHEMBL189231 IC50 = 3.0 nM 8.52
CHEMBL187340 IC50 = 4.0 nM 8.40
CHEMBL188268 IC50 = 4.0 nM 8.40
CHEMBL188433 IC50 = 6.0 nM 8.22
CHEMBL360219 IC50 = 7.0 nM 8.15
CHEMBL364413 IC50 = 8.0 nM 8.10
CHEMBL188620 IC50 = 9.0 nM 8.05
CHEMBL365832 IC50 = 9.0 nM 8.05
CHEMBL363258 IC50 = 13.0 nM 7.89
CHEMBL363054 IC50 = 17.0 nM 7.77
CHEMBL189773 IC50 = 22.0 nM 7.66
CHEMBL188240 IC50 = 174.0 nM 6.76
CHEMBL363990 IC50 = 209.0 nM 6.68
CHEMBL365072 IC50 = 229.0 nM 6.64
CHEMBL191105 IC50 = 617.0 nM 6.21
CHEMBL186343 IC50 = 813.0 nM 6.09
CHEMBL187985 IC50 = 2240.0 nM 5.65
CHEMBL371391 IC50 = 10000.0 nM 5.00