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Assay Detail

CHEMBL4824876

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

Binding
Inhibition of IDO1 in IFNgamma-stimulated human HeLa cells preincubated for 2 hrs followed by recombinant human IFNgamma stimulation and measured after 18 hrs by fluorescence based microplate reader assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Indoleamine 2,3-dioxygenase 1 (CHEMBL4685)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Conformational-Analysis-Guided Discovery of 2,3-Disubstituted Pyridine IDO1 Inhibitors.
Cherney EC, Zhang L, Guo W, Huang A, Williams D, Seitz S, Shan W, Zhu X, Gullo-Brown J, Maley D, Lin TA, Hunt JT, Huang C, Yang Z, D'Arienzo CJ, Discenza LN, Ranasinghe A, Grubb MF, Traeger SC, Li X, Johnston KA, Kopcho L, Fereshteh M, Foster KA, Stefanski K, Delpy D, Dhar G, Anandam A, Mahankali S, Padmanabhan S, Rajanna P, Murali V, Mariappan TT, Pattasseri S, Nimje RY, Hong Z, Kempson J, Rampulla R, Mathur A, Gupta A, Borzilleri R, Vite G, Balog A.
ACS Med Chem Lett (2021) 12 : 1143 -1150
PubMed 34267885 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 7.97 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4786690 1 8.70
CHEMBL4868709 1 8.70
CHEMBL4845988 1 8.70
CHEMBL4848094 1 8.70
CHEMBL4851220 1 8.70
CHEMBL4860353 1 8.52
CHEMBL4877466 1 8.40
CHEMBL4859400 1 8.30
CHEMBL4861763 1 8.15
CHEMBL4859579 1 7.92
CHEMBL4860098 1 7.85
CHEMBL4849714 1 7.72
CHEMBL4860594 1 7.58
CHEMBL4847982 1 7.40
CHEMBL4849654 1 7.37
CHEMBL4857086 1 7.32
CHEMBL4854619 1 7.10
CHEMBL4873558 1 6.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4786690 IC50 = 2.0 nM 8.70
CHEMBL4868709 IC50 = 2.0 nM 8.70
CHEMBL4845988 IC50 = 2.0 nM 8.70
CHEMBL4848094 IC50 = 2.0 nM 8.70
CHEMBL4851220 IC50 = 2.0 nM 8.70
CHEMBL4860353 IC50 = 3.0 nM 8.52
CHEMBL4877466 IC50 = 4.0 nM 8.40
CHEMBL4859400 IC50 = 5.0 nM 8.30
CHEMBL4861763 IC50 = 7.0 nM 8.15
CHEMBL4859579 IC50 = 12.0 nM 7.92
CHEMBL4860098 IC50 = 14.0 nM 7.85
CHEMBL4849714 IC50 = 19.0 nM 7.72
CHEMBL4860594 IC50 = 26.0 nM 7.58
CHEMBL4847982 IC50 = 40.0 nM 7.40
CHEMBL4849654 IC50 = 43.0 nM 7.37
CHEMBL4857086 IC50 = 48.0 nM 7.32
CHEMBL4854619 IC50 = 80.0 nM 7.10
CHEMBL4873558 IC50 = 475.0 nM 6.32