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Assay Detail

CHEMBL5168687

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

Binding
Inhibition of recombinant N-terminal GST tagged AKT2 (108 to 479 end residues) (unknown origin) catalytic domain expressed in Sf21 cells using peptide substrate incubated for 1 hr in presence of ATP by caliper off-chip mobility shift assay
43
Total Activities
43
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

RAC-gamma serine/threonine-protein kinase (CHEMBL4816)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Clinical Candidate NTQ1062 as a Potent and Bioavailable Akt Inhibitor for the Treatment of Human Tumors.
Ma C, Wu J, Wang L, Ji X, Wu Y, Miao L, Chen D, Zhang L, Wu Y, Feng H, Tang Y, Zhou Q, Pei J, Yang X, Xu D, You Q, Xie Y.
J Med Chem (2022) 65 : 8144 -8168
PubMed 35679512 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 43 8.48 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5182446 1 10.00
CHEMBL5197007 1 10.00
CHEMBL5169427 1 10.00
CHEMBL5195745 1 9.70
CHEMBL5175628 1 9.70
CHEMBL5175332 1 9.70
CHEMBL5190230 1 9.70
CHEMBL5180219 1 9.70
CHEMBL5177491 1 9.52
CHEMBL5206905 1 9.52
CHEMBL5195664 1 9.40
CHEMBL5189707 1 9.40
CHEMBL5193325 1 9.30
CHEMBL5187172 1 9.30
CHEMBL5171561 1 9.30
CHEMBL5187508 1 9.15
CHEMBL5189610 1 9.00
CHEMBL5192188 1 8.92
CHEMBL5199199 1 8.92
CHEMBL5187287 1 8.80
CHEMBL5190647 1 8.59
CHEMBL5174965 1 8.36
CHEMBL5172419 1 8.18
CHEMBL5185923 1 8.13
CHEMBL5187546 1 8.13
CHEMBL5188472 1 8.12
CHEMBL5175305 1 8.07
CHEMBL5194492 1 8.04
CHEMBL5169446 1 7.92
CHEMBL5188354 1 7.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5182446 IC50 = 0.1 nM 10.00
CHEMBL5169427 IC50 = 0.1 nM 10.00
CHEMBL5197007 IC50 = 0.1 nM 10.00
CHEMBL5195745 IC50 = 0.2 nM 9.70
CHEMBL5175628 IC50 = 0.2 nM 9.70
CHEMBL5175332 IC50 = 0.2 nM 9.70
CHEMBL5190230 IC50 = 0.2 nM 9.70
CHEMBL5180219 IC50 = 0.2 nM 9.70
CHEMBL5177491 IC50 = 0.3 nM 9.52
CHEMBL5206905 IC50 = 0.3 nM 9.52
CHEMBL5195664 IC50 = 0.4 nM 9.40
CHEMBL5189707 IC50 = 0.4 nM 9.40
CHEMBL5193325 IC50 = 0.5 nM 9.30
CHEMBL5171561 IC50 = 0.5 nM 9.30
CHEMBL5187172 IC50 = 0.5 nM 9.30
CHEMBL5187508 IC50 = 0.7 nM 9.15
CHEMBL5189610 IC50 = 1.0 nM 9.00
CHEMBL5192188 IC50 = 1.2 nM 8.92
CHEMBL5199199 IC50 = 1.2 nM 8.92
CHEMBL5187287 IC50 = 1.6 nM 8.80
CHEMBL5190647 IC50 = 2.6 nM 8.59
CHEMBL5174965 IC50 = 4.4 nM 8.36
CHEMBL5172419 IC50 = 6.6 nM 8.18
CHEMBL5185923 IC50 = 7.4 nM 8.13
CHEMBL5187546 IC50 = 7.4 nM 8.13
CHEMBL5188472 IC50 = 7.5 nM 8.12
CHEMBL5175305 IC50 = 8.5 nM 8.07
CHEMBL5194492 IC50 = 9.1 nM 8.04
CHEMBL5169446 IC50 = 12.0 nM 7.92
CHEMBL5188354 IC50 = 13.0 nM 7.89
CHEMBL5198109 IC50 = 18.0 nM 7.75
CHEMBL2177390 IPATASERTIB IC50 = 22.0 nM 7.66
CHEMBL5181964 IC50 = 24.0 nM 7.62
CHEMBL5193935 IC50 = 42.0 nM 7.38
CHEMBL5181308 IC50 = 60.0 nM 7.22
CHEMBL5183601 IC50 = 61.0 nM 7.21
CHEMBL5200967 IC50 = 135.0 nM 6.87
CHEMBL5189748 IC50 = 160.0 nM 6.80
CHEMBL5205187 IC50 = 212.0 nM 6.67
CHEMBL5176995 IC50 = 661.0 nM 6.18
CHEMBL5177946 IC50 = 953.0 nM 6.02
CHEMBL5206091 IC50 > 1000.0 nM -
CHEMBL5172329 IC50 > 1000.0 nM -