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Assay Detail

CHEMBL1103720

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

Binding
Inhibition of PKA
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

The identification of 8,9-dimethoxy-5-(2-aminoalkoxy-pyridin-3-yl)-benzo[c][2,7]naphthyridin-4-ylamines as potent inhibitors of 3-phosphoinositide-dependent kinase-1 (PDK-1).
Nittoli T, Dushin RG, Ingalls C, Cheung K, Floyd MB, Fraser H, Olland A, Hu Y, Grosu G, Han X, Arndt K, Guo B, Wissner A.
Eur J Med Chem (2010) 45 : 1379 -1386
PubMed 20074837 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 7.14 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1096271 1 7.75
CHEMBL1095621 1 7.50
CHEMBL1095622 1 7.44
CHEMBL1097972 1 7.39
CHEMBL1094320 1 7.35
CHEMBL1095612 1 7.27
CHEMBL1097956 1 7.23
CHEMBL1095278 1 7.18
CHEMBL1098302 1 7.17
CHEMBL1097602 1 7.11
CHEMBL1095931 1 7.10
CHEMBL1097955 1 7.07
CHEMBL1094321 1 6.95
CHEMBL1097604 1 6.92
CHEMBL1095279 1 6.91
CHEMBL1097973 1 6.86
CHEMBL1095285 1 6.85
CHEMBL1094637 1 6.42
CHEMBL1095294 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1096271 IC50 = 18.0 nM 7.75
CHEMBL1095621 IC50 = 32.0 nM 7.50
CHEMBL1095622 IC50 = 36.0 nM 7.44
CHEMBL1097972 IC50 = 41.0 nM 7.39
CHEMBL1094320 IC50 = 45.0 nM 7.35
CHEMBL1095612 IC50 = 54.0 nM 7.27
CHEMBL1097956 IC50 = 59.0 nM 7.23
CHEMBL1095278 IC50 = 66.0 nM 7.18
CHEMBL1098302 IC50 = 68.0 nM 7.17
CHEMBL1097602 IC50 = 77.0 nM 7.11
CHEMBL1095931 IC50 = 79.0 nM 7.10
CHEMBL1097955 IC50 = 86.0 nM 7.07
CHEMBL1094321 IC50 = 113.0 nM 6.95
CHEMBL1097604 IC50 = 120.0 nM 6.92
CHEMBL1095279 IC50 = 123.0 nM 6.91
CHEMBL1097973 IC50 = 138.0 nM 6.86
CHEMBL1095285 IC50 = 142.0 nM 6.85
CHEMBL1094637 IC50 = 385.0 nM 6.42
CHEMBL1095294 IC50 < 31.0 nM -