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Assay Detail

CHEMBL5142246

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

Binding
Inhibition of IDO1 (unknown origin) assessed as reduction in kynurenine production using L-tryptophan as substrate incubated for 1 hr by absorbance based microplate reader analysis
14
Total Activities
14
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 1-(Hetero)aryl-β-carboline Derivatives as IDO1/TDO Dual Inhibitors with Antidepressant Activity.
Zhang Y, Li Y, Chen X, Chen X, Chen C, Wang L, Dong X, Wang G, Gu R, Li F, Han F, Chen D.
J Med Chem (2022) 65 : 11214 -11228
PubMed 35938398 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.18 6.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4086143 PF-06840003 1.0 1 6.43
CHEMBL274452 1 5.45
CHEMBL5172850 1 5.30
CHEMBL5187479 1 5.12
CHEMBL5207121 1 5.08
CHEMBL2030639 1 5.07
CHEMBL5188549 1 4.86
CHEMBL5195156 1 4.78
CHEMBL5207671 1 4.49
CHEMBL5180636 1 -
CHEMBL5185419 1 -
CHEMBL5184595 1 -
CHEMBL5194494 1 -
CHEMBL38596 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4086143 PF-06840003 IC50 = 370.0 nM 6.43
CHEMBL274452 IC50 = 3530.0 nM 5.45
CHEMBL5172850 IC50 = 4950.0 nM 5.30
CHEMBL5187479 IC50 = 7580.0 nM 5.12
CHEMBL5207121 IC50 = 8280.0 nM 5.08
CHEMBL2030639 IC50 = 8440.0 nM 5.07
CHEMBL5188549 IC50 = 13880.0 nM 4.86
CHEMBL5195156 IC50 = 16490.0 nM 4.78
CHEMBL5207671 IC50 = 32710.0 nM 4.49
CHEMBL5180636 IC50 > 50000.0 nM -
CHEMBL5185419 IC50 > 50000.0 nM -
CHEMBL5184595 IC50 > 50000.0 nM -
CHEMBL5194494 IC50 > 50000.0 nM -
CHEMBL38596 IC50 > 50000.0 nM -