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Assay Detail

CHEMBL4831257

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

Binding
Inhibition of N-terminal His6-tagged human p70S6k T412E mutant (1 to 421 residues) expressed in Sf21 cells using FITC-AHA-AKRRRLSSLRA-OH as substrate incubated for 90 mins by mobility shift assay
48
Total Activities
48
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf21
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Ribosomal protein S6 kinase beta-1 (CHEMBL4501)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of Clinical Candidate M2698, a Dual p70S6K and Akt Inhibitor, for Treatment of PAM Pathway-Altered Cancers.
DeSelm L, Huck B, Lan R, Neagu C, Potnick J, Xiao Y, Chen X, Jones R, Richardson TE, Heasley BH, Haxell T, Moore J, Tian H, Georgi K, Rohdich F, Sutton A, Johnson T, Mochalkin I, Jackson J, Lin J, Crowley L, Machl A, Clark A, Wilker E, Sherer B, Goutopoulos A.
J Med Chem (2021) 64 : 14603 -14619
PubMed 34596404 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 48 7.86 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3685329 1 9.22
CHEMBL3670464 1 9.10
CHEMBL4860970 1 9.00
CHEMBL4871853 1 9.00
CHEMBL3675415 1 9.00
CHEMBL4871106 RUPITASERTIB 2.0 1 8.96
CHEMBL4855657 1 8.89
CHEMBL4876446 1 8.85
CHEMBL4856439 1 8.70
CHEMBL3675355 1 8.70
CHEMBL4869229 1 8.70
CHEMBL4854144 1 8.70
CHEMBL4851020 1 8.62
CHEMBL3675442 1 8.59
CHEMBL4846712 1 8.54
CHEMBL3670413 1 8.54
CHEMBL4878044 1 8.21
CHEMBL4875416 1 8.10
CHEMBL3675344 1 7.96
CHEMBL3675354 1 7.62
CHEMBL4846770 1 7.60
CHEMBL3675353 1 7.58
CHEMBL3680423 1 7.55
CHEMBL4853030 1 7.52
CHEMBL3670457 1 7.52
CHEMBL3680434 1 7.51
CHEMBL3675337 1 7.50
CHEMBL3675340 1 7.41
CHEMBL3675343 1 7.38
CHEMBL3675333 1 7.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3685329 IC50 = 0.6 nM 9.22
CHEMBL3670464 IC50 = 0.8 nM 9.10
CHEMBL4871853 IC50 = 1.0 nM 9.00
CHEMBL3675415 IC50 = 1.0 nM 9.00
CHEMBL4860970 IC50 = 1.0 nM 9.00
CHEMBL4871106 RUPITASERTIB IC50 = 1.1 nM 8.96
CHEMBL4855657 IC50 = 1.3 nM 8.89
CHEMBL4876446 IC50 = 1.4 nM 8.85
CHEMBL4856439 IC50 = 2.0 nM 8.70
CHEMBL3675355 IC50 = 2.0 nM 8.70
CHEMBL4869229 IC50 = 2.0 nM 8.70
CHEMBL4854144 IC50 = 2.0 nM 8.70
CHEMBL4851020 IC50 = 2.4 nM 8.62
CHEMBL3675442 IC50 = 2.6 nM 8.59
CHEMBL3670413 IC50 = 2.9 nM 8.54
CHEMBL4846712 IC50 = 2.9 nM 8.54
CHEMBL4878044 IC50 = 6.2 nM 8.21
CHEMBL4875416 IC50 = 8.0 nM 8.10
CHEMBL3675344 IC50 = 11.0 nM 7.96
CHEMBL3675354 IC50 = 24.0 nM 7.62
CHEMBL4846770 IC50 = 25.0 nM 7.60
CHEMBL3675353 IC50 = 26.0 nM 7.58
CHEMBL3680423 IC50 = 28.0 nM 7.55
CHEMBL3670457 IC50 = 30.0 nM 7.52
CHEMBL4853030 IC50 = 30.0 nM 7.52
CHEMBL3680434 IC50 = 31.0 nM 7.51
CHEMBL3675337 IC50 = 32.0 nM 7.50
CHEMBL3675340 IC50 = 39.0 nM 7.41
CHEMBL3675343 IC50 = 42.0 nM 7.38
CHEMBL3675333 IC50 = 55.0 nM 7.26
CHEMBL4857965 IC50 = 65.0 nM 7.19
CHEMBL3680521 IC50 = 84.0 nM 7.08
CHEMBL3670427 IC50 = 92.0 nM 7.04
CHEMBL3639742 IC50 = 102.0 nM 6.99
CHEMBL3680537 IC50 = 102.0 nM 6.99
CHEMBL3675357 IC50 = 104.0 nM 6.98
CHEMBL4870165 IC50 = 160.0 nM 6.80
CHEMBL3675347 IC50 = 183.0 nM 6.74
CHEMBL3675352 IC50 = 530.0 nM 6.28
CHEMBL3675367 IC50 = 644.0 nM 6.19
CHEMBL4878255 IC50 = 973.0 nM 6.01
CHEMBL4847586 IC50 > 10000.0 nM -
CHEMBL4875216 IC50 > 10000.0 nM -
CHEMBL4861175 IC50 > 10000.0 nM -
CHEMBL4853114 IC50 > 10000.0 nM -
CHEMBL4859445 IC50 > 1000.0 nM -
CHEMBL102726 IC50 > 10000.0 nM -
CHEMBL4872249 IC50 > 10000.0 nM -