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Assay Detail

CHEMBL1104613

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

Binding
Inhibition of human mTOR (1360-2549 amino acids) expressed in HEK293 cells
ChEMBL ↗
49
Total Activities
49
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Serine/threonine-protein kinase mTOR (CHEMBL2842) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of 4-morpholino-6-aryl-1H-pyrazolo[3,4-d]pyrimidines as highly potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): optimization of the 6-aryl substituent.
Verheijen JC, Richard DJ, Curran K, Kaplan J, Lefever M, Nowak P, Malwitz DJ, Brooijmans N, Toral-Barza L, Zhang WG, Lucas J, Hollander I, Ayral-Kaloustian S, Mansour TS, Yu K, Zask A.
J Med Chem (2009) 52 : 8010 -8024
PubMed 19894727 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 49 8.41 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1098245 — — 1 10.00
CHEMBL1095932 — — 1 9.70
CHEMBL1094981 — — 1 9.52
CHEMBL556947 — — 1 9.52
CHEMBL1097896 — — 1 9.52
CHEMBL1098244 — — 1 9.52
CHEMBL1095627 — — 1 9.40
CHEMBL551440 — — 1 9.40
CHEMBL1097942 — — 1 9.30
CHEMBL562999 — — 1 9.30
CHEMBL1098242 — — 1 9.30
CHEMBL550972 — — 1 9.30
CHEMBL563985 — — 1 9.30
CHEMBL561907 — — 1 9.22
CHEMBL1098243 — — 1 9.22
CHEMBL1098248 — — 1 9.22
CHEMBL1097902 — — 1 9.15
CHEMBL1095933 — — 1 9.15
CHEMBL1098246 — — 1 9.15
CHEMBL1098247 — — 1 9.10
CHEMBL1097901 — — 1 9.10
CHEMBL1098306 — — 1 9.10
CHEMBL1097893 — — 1 8.85
CHEMBL552532 — — 1 8.82
CHEMBL1097900 — — 1 8.62
CHEMBL1097895 — — 1 8.59
CHEMBL1098305 — — 1 8.57
CHEMBL1095626 — — 1 8.34
CHEMBL561103 — — 1 8.34
CHEMBL1097894 — — 1 8.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1098245 — IC50 = 0.1 nM 10.00
CHEMBL1095932 — IC50 = 0.2 nM 9.70
CHEMBL556947 — IC50 = 0.3 nM 9.52
CHEMBL1097896 — IC50 = 0.3 nM 9.52
CHEMBL1098244 — IC50 = 0.3 nM 9.52
CHEMBL1094981 — IC50 = 0.3 nM 9.52
CHEMBL1095627 — IC50 = 0.4 nM 9.40
CHEMBL551440 — IC50 = 0.4 nM 9.40
CHEMBL1097942 — IC50 = 0.5 nM 9.30
CHEMBL562999 — IC50 = 0.5 nM 9.30
CHEMBL1098242 — IC50 = 0.5 nM 9.30
CHEMBL550972 — IC50 = 0.5 nM 9.30
CHEMBL563985 — IC50 = 0.5 nM 9.30
CHEMBL1098248 — IC50 = 0.6 nM 9.22
CHEMBL561907 — IC50 = 0.6 nM 9.22
CHEMBL1098243 — IC50 = 0.6 nM 9.22
CHEMBL1097902 — IC50 = 0.7 nM 9.15
CHEMBL1095933 — IC50 = 0.7 nM 9.15
CHEMBL1098246 — IC50 = 0.7 nM 9.15
CHEMBL1098247 — IC50 = 0.8 nM 9.10
CHEMBL1097901 — IC50 = 0.8 nM 9.10
CHEMBL1098306 — IC50 = 0.8 nM 9.10
CHEMBL1097893 — IC50 = 1.4 nM 8.85
CHEMBL552532 — IC50 = 1.5 nM 8.82
CHEMBL1097900 — IC50 = 2.4 nM 8.62
CHEMBL1097895 — IC50 = 2.6 nM 8.59
CHEMBL1098305 — IC50 = 2.7 nM 8.57
CHEMBL1095626 — IC50 = 4.6 nM 8.34
CHEMBL561103 — IC50 = 4.6 nM 8.34
CHEMBL1097894 — IC50 = 4.8 nM 8.32
CHEMBL1095618 — IC50 = 9.6 nM 8.02
CHEMBL1098301 — IC50 = 12.0 nM 7.92
CHEMBL1095945 — IC50 = 16.0 nM 7.80
CHEMBL1098619 — IC50 = 16.0 nM 7.80
CHEMBL1098300 — IC50 = 20.0 nM 7.70
CHEMBL1097897 — IC50 = 23.0 nM 7.64
CHEMBL1095946 — IC50 = 23.0 nM 7.64
CHEMBL1097261 — IC50 = 27.0 nM 7.57
CHEMBL1097898 — IC50 = 65.0 nM 7.19
CHEMBL1097263 — IC50 = 73.0 nM 7.14
CHEMBL1097603 — IC50 = 76.0 nM 7.12
CHEMBL1097561 — IC50 = 84.0 nM 7.08
CHEMBL1097262 — IC50 = 111.0 nM 6.96
CHEMBL1098310 — IC50 = 113.0 nM 6.95
CHEMBL1097899 — IC50 = 125.0 nM 6.90
CHEMBL1098311 — IC50 = 145.0 nM 6.84
CHEMBL1095623 — IC50 = 170.0 nM 6.77
CHEMBL1095625 — IC50 = 200.0 nM 6.70
CHEMBL1095281 — IC50 = 480.0 nM 6.32