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Assay Detail

CHEMBL5218088

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

Binding
Inhibition of human ADCY10 assessed as cAMP accumulation preincubated for 15 mins followed by substrate addition using alpha-32P labelled ATP as substrate by sequential chromatographic analysis
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adenylate cyclase type 10 (CHEMBL5854)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, Synthesis, and Pharmacological Evaluation of Second-Generation Soluble Adenylyl Cyclase (sAC, ADCY10) Inhibitors with Slow Dissociation Rates.
Miller M, Rossetti T, Ferreira J, Ghanem L, Balbach M, Kaur N, Levin LR, Buck J, Kehr M, Coquille S, van den Heuvel J, Steegborn C, Fushimi M, Finkin-Groner E, Myers RW, Kargman S, Liverton NJ, Huggins DJ, Meinke PT.
J Med Chem (2022) 65 : 15208 -15226
PubMed 36346696 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 7.38 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5220685 1 9.00
CHEMBL5218878 1 8.68
CHEMBL5218552 1 8.66
CHEMBL5218615 1 8.62
CHEMBL5219830 1 8.48
CHEMBL5219579 1 8.48
CHEMBL5218698 1 8.41
CHEMBL5218702 1 8.40
CHEMBL5220647 1 8.34
CHEMBL5219443 1 8.26
CHEMBL5220895 1 8.17
CHEMBL5220347 1 8.11
CHEMBL5220723 1 7.91
CHEMBL5219922 1 7.77
CHEMBL5219530 1 7.68
CHEMBL5220632 1 7.62
CHEMBL5221008 1 7.19
CHEMBL5220075 1 7.17
CHEMBL5221093 1 7.06
CHEMBL5219193 1 6.95
CHEMBL4854762 1 6.80
CHEMBL4867202 1 6.46
CHEMBL5219159 1 6.41
CHEMBL5219933 1 6.36
CHEMBL5220308 1 6.33
CHEMBL5219011 1 6.14
CHEMBL5218555 1 6.08
CHEMBL4874934 1 5.99
CHEMBL5218712 1 5.91
CHEMBL5219751 1 5.73

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5220685 IC50 = 1.0 nM 9.00
CHEMBL5218878 IC50 = 2.1 nM 8.68
CHEMBL5218552 IC50 = 2.2 nM 8.66
CHEMBL5218615 IC50 = 2.4 nM 8.62
CHEMBL5219830 IC50 = 3.33 nM 8.48
CHEMBL5219579 IC50 = 3.3 nM 8.48
CHEMBL5218698 IC50 = 3.9 nM 8.41
CHEMBL5218702 IC50 = 4.0 nM 8.40
CHEMBL5220647 IC50 = 4.6 nM 8.34
CHEMBL5219443 IC50 = 5.5 nM 8.26
CHEMBL5220895 IC50 = 6.7 nM 8.17
CHEMBL5220347 IC50 = 7.8 nM 8.11
CHEMBL5220723 IC50 = 12.3 nM 7.91
CHEMBL5219922 IC50 = 16.9 nM 7.77
CHEMBL5219530 IC50 = 21.0 nM 7.68
CHEMBL5220632 IC50 = 24.2 nM 7.62
CHEMBL5221008 IC50 = 64.0 nM 7.19
CHEMBL5220075 IC50 = 67.0 nM 7.17
CHEMBL5221093 IC50 = 87.1 nM 7.06
CHEMBL5219193 IC50 = 112.0 nM 6.95
CHEMBL4854762 IC50 = 159.0 nM 6.80
CHEMBL4867202 IC50 = 351.0 nM 6.46
CHEMBL5219159 IC50 = 389.0 nM 6.41
CHEMBL5219933 IC50 = 436.0 nM 6.36
CHEMBL5220308 IC50 = 469.0 nM 6.33
CHEMBL5219011 IC50 = 716.0 nM 6.14
CHEMBL5218555 IC50 = 829.0 nM 6.08
CHEMBL4874934 IC50 = 1024.0 nM 5.99
CHEMBL5218712 IC50 = 1245.0 nM 5.91
CHEMBL5219751 IC50 = 1876.0 nM 5.73
CHEMBL5220138 IC50 = 2577.0 nM 5.59