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Assay Detail

CHEMBL4843237

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

Binding
Inhibition of IDO1 in human HeLa cells using tryptophan as substrate incubated for 24 hrs by RFMS assay
63
Total Activities
62
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

Discovery of IACS-9779 and IACS-70465 as Potent Inhibitors Targeting Indoleamine 2,3-Dioxygenase 1 (IDO1) Apoenzyme.
Hamilton MM, Mseeh F, McAfoos TJ, Leonard PG, Reyna NJ, Harris AL, Xu A, Han M, Soth MJ, Czako B, Theroff JP, Mandal PK, Burke JP, Virgin-Downey B, Petrocchi A, Pfaffinger D, Rogers NE, Parker CA, Yu SS, Jiang Y, Krapp S, Lammens A, Trevitt G, Tremblay MR, Mikule K, Wilcoxen K, Cross JB, Jones P, Marszalek JR, Lewis RT.
J Med Chem (2021) 64 : 11302 -11329
PubMed 34292726 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 63 7.94 9.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4873747 1 9.28
CHEMBL4856710 1 9.22
CHEMBL4858888 1 9.16
CHEMBL4849690 1 9.04
CHEMBL4875089 1 9.00
CHEMBL4868112 1 8.85
CHEMBL4872522 1 8.80
CHEMBL4861332 1 8.77
CHEMBL4859064 2 8.66
CHEMBL4866976 1 8.59
CHEMBL4866113 1 8.59
CHEMBL4863359 1 8.47
CHEMBL4846356 1 8.44
CHEMBL4869547 1 8.41
CHEMBL4856417 1 8.40
CHEMBL4873928 1 8.38
CHEMBL4853672 1 8.36
CHEMBL4858219 1 8.34
CHEMBL4849414 1 8.28
CHEMBL4866916 1 8.28
CHEMBL4854742 1 8.21
CHEMBL4846874 1 8.21
CHEMBL4852566 1 8.21
CHEMBL4878766 1 8.20
CHEMBL4853036 1 8.16
CHEMBL4873803 1 8.15
CHEMBL4872039 1 8.15
CHEMBL4848111 1 8.08
CHEMBL4871068 1 8.08
CHEMBL4845961 1 8.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4873747 IC50 = 0.52 nM 9.28
CHEMBL4856710 IC50 = 0.6 nM 9.22
CHEMBL4858888 IC50 = 0.69 nM 9.16
CHEMBL4849690 IC50 = 0.92 nM 9.04
CHEMBL4875089 IC50 = 1.0 nM 9.00
CHEMBL4868112 IC50 = 1.4 nM 8.85
CHEMBL4872522 IC50 = 1.6 nM 8.80
CHEMBL4861332 IC50 = 1.7 nM 8.77
CHEMBL4859064 IC50 = 2.2 nM 8.66
CHEMBL4866113 IC50 = 2.6 nM 8.59
CHEMBL4866976 IC50 = 2.6 nM 8.59
CHEMBL4859064 IC50 = 2.8 nM 8.55
CHEMBL4863359 IC50 = 3.4 nM 8.47
CHEMBL4846356 IC50 = 3.6 nM 8.44
CHEMBL4869547 IC50 = 3.9 nM 8.41
CHEMBL4856417 IC50 = 4.0 nM 8.40
CHEMBL4873928 IC50 = 4.2 nM 8.38
CHEMBL4853672 IC50 = 4.4 nM 8.36
CHEMBL4858219 IC50 = 4.6 nM 8.34
CHEMBL4866916 IC50 = 5.2 nM 8.28
CHEMBL4849414 IC50 = 5.3 nM 8.28
CHEMBL4852566 IC50 = 6.2 nM 8.21
CHEMBL4854742 IC50 = 6.2 nM 8.21
CHEMBL4846874 IC50 = 6.1 nM 8.21
CHEMBL4878766 IC50 = 6.3 nM 8.20
CHEMBL4853036 IC50 = 6.9 nM 8.16
CHEMBL4873803 IC50 = 7.0 nM 8.15
CHEMBL4872039 IC50 = 7.0 nM 8.15
CHEMBL4845961 IC50 = 8.3 nM 8.08
CHEMBL4848111 IC50 = 8.4 nM 8.08
CHEMBL4871068 IC50 = 8.4 nM 8.08
CHEMBL4848514 IC50 = 8.8 nM 8.06
CHEMBL4872488 IC50 = 9.1 nM 8.04
CHEMBL4864639 IC50 = 9.2 nM 8.04
CHEMBL4852532 IC50 = 9.9 nM 8.00
CHEMBL3545369 EPACADOSTAT IC50 = 11.0 nM 7.96
CHEMBL4862584 IC50 = 12.0 nM 7.92
CHEMBL4872803 IC50 = 14.0 nM 7.85
CHEMBL4873892 IC50 = 18.0 nM 7.75
CHEMBL4862755 IC50 = 19.0 nM 7.72
CHEMBL4861936 IC50 = 19.0 nM 7.72
CHEMBL4865079 IC50 = 19.0 nM 7.72
CHEMBL4878988 IC50 = 22.0 nM 7.66
CHEMBL4870664 IC50 = 23.0 nM 7.64
CHEMBL4853212 IC50 = 26.0 nM 7.58
CHEMBL4868833 IC50 = 28.0 nM 7.55
CHEMBL4865106 IC50 = 30.0 nM 7.52
CHEMBL4856573 IC50 = 32.0 nM 7.50
CHEMBL4877654 IC50 = 33.0 nM 7.48
CHEMBL4846783 IC50 = 33.0 nM 7.48