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Assay Detail

CHEMBL4367261

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Binding
Inhibition of purified human IDO1 using L-tryptophan as substrate preincubated for 5 mins followed by substrate addition and measured after 15 mins by spectrophotometric method
ChEMBL ↗
87
Total Activities
87
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

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

Publication

Discovery of Clinical Candidate (1R,4r)-4-((R)-2-((S)-6-Fluoro-5H-imidazo[5,1-a]isoindol-5-yl)-1-hydroxyethyl)cyclohexan-1-ol (Navoximod), a Potent and Selective Inhibitor of Indoleamine 2,3-Dioxygenase 1.
Kumar S, Waldo JP, Jaipuri FA, Marcinowicz A, Van Allen C, Adams J, Kesharwani T, Zhang X, Metz R, Oh AJ, Harris SF, Mautino MR.
J Med Chem (2019) 62 : 6705 -6733
PubMed 31264862 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 87 5.98 7.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3752060 — — 1 7.68
CHEMBL3989951 NAVOXIMOD 2.0 1 7.55
CHEMBL3753837 — — 1 7.52
CHEMBL4537319 — — 1 7.51
CHEMBL4542242 — — 1 7.40
CHEMBL4446572 — — 1 7.38
CHEMBL4577440 — — 1 7.35
CHEMBL4570289 — — 1 7.34
CHEMBL4450473 — — 1 7.30
CHEMBL3629569 — — 1 7.22
CHEMBL4550278 — — 1 7.14
CHEMBL4530496 — — 1 7.05
CHEMBL4576829 — — 1 7.00
CHEMBL3752711 — — 1 6.96
CHEMBL4454031 — — 1 6.87
CHEMBL4467319 — — 1 6.85
CHEMBL4594197 — — 1 6.80
CHEMBL4476312 — — 1 6.70
CHEMBL4517185 — — 1 6.70
CHEMBL4546052 — — 1 6.68
CHEMBL4559452 — — 1 6.64
CHEMBL4562289 — — 1 6.58
CHEMBL4461858 — — 1 6.55
CHEMBL4579820 — — 1 6.52
CHEMBL4453343 — — 1 6.48
CHEMBL4449872 — — 1 6.43
CHEMBL4563021 — — 1 6.38
CHEMBL4540038 — — 1 6.36
CHEMBL4455007 — — 1 6.31
CHEMBL4543526 — — 1 6.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3752060 — IC50 = 21.0 nM 7.68
CHEMBL3989951 NAVOXIMOD IC50 = 28.0 nM 7.55
CHEMBL3753837 — IC50 = 30.0 nM 7.52
CHEMBL4537319 — IC50 = 31.0 nM 7.51
CHEMBL4542242 — IC50 = 40.0 nM 7.40
CHEMBL4446572 — IC50 = 42.0 nM 7.38
CHEMBL4577440 — IC50 = 45.0 nM 7.35
CHEMBL4570289 — IC50 = 46.0 nM 7.34
CHEMBL4450473 — IC50 = 50.0 nM 7.30
CHEMBL3629569 — IC50 = 60.0 nM 7.22
CHEMBL4550278 — IC50 = 72.0 nM 7.14
CHEMBL4530496 — IC50 = 90.0 nM 7.05
CHEMBL4576829 — IC50 = 100.0 nM 7.00
CHEMBL3752711 — IC50 = 110.0 nM 6.96
CHEMBL4454031 — IC50 = 135.0 nM 6.87
CHEMBL4467319 — IC50 = 140.0 nM 6.85
CHEMBL4594197 — IC50 = 160.0 nM 6.80
CHEMBL4476312 — IC50 = 200.0 nM 6.70
CHEMBL4517185 — IC50 = 200.0 nM 6.70
CHEMBL4546052 — IC50 = 210.0 nM 6.68
CHEMBL4559452 — IC50 = 230.0 nM 6.64
CHEMBL4562289 — IC50 = 260.0 nM 6.58
CHEMBL4461858 — IC50 = 280.0 nM 6.55
CHEMBL4579820 — IC50 = 300.0 nM 6.52
CHEMBL4453343 — IC50 = 330.0 nM 6.48
CHEMBL4449872 — IC50 = 370.0 nM 6.43
CHEMBL4563021 — IC50 = 420.0 nM 6.38
CHEMBL4540038 — IC50 = 440.0 nM 6.36
CHEMBL4455007 — IC50 = 490.0 nM 6.31
CHEMBL4543526 — IC50 = 600.0 nM 6.22
CHEMBL4552010 — IC50 = 610.0 nM 6.21
CHEMBL4576216 — IC50 = 640.0 nM 6.19
CHEMBL4461262 — IC50 = 670.0 nM 6.17
CHEMBL4473619 — IC50 = 700.0 nM 6.16
CHEMBL4445081 — IC50 = 760.0 nM 6.12
CHEMBL4528916 — IC50 = 790.0 nM 6.10
CHEMBL4557815 — IC50 = 810.0 nM 6.09
CHEMBL4534741 — IC50 = 906.0 nM 6.04
CHEMBL4539142 — IC50 = 960.0 nM 6.02
CHEMBL4551141 — IC50 = 1100.0 nM 5.96
CHEMBL4542931 — IC50 = 1200.0 nM 5.92
CHEMBL4467206 — IC50 = 1500.0 nM 5.82
CHEMBL457063 — IC50 = 1700.0 nM 5.77
CHEMBL4439222 — IC50 = 1700.0 nM 5.77
CHEMBL4466768 — IC50 = 1700.0 nM 5.77
CHEMBL4439809 — IC50 = 1800.0 nM 5.75
CHEMBL4449551 — IC50 = 1900.0 nM 5.72
CHEMBL4571106 — IC50 = 2400.0 nM 5.62
CHEMBL4566253 — IC50 = 2500.0 nM 5.60
CHEMBL4443852 — IC50 = 2900.0 nM 5.54