Assay Detail

CHEMBL4834191

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Binding

Inhibition of TNF-alpha in thapsigargin stimulated human whole blood

ChEMBL ↗

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Target

Tumor necrosis factor (CHEMBL1825) ↗

Open DB target context

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Tumor necrosis factor (CHEMBL1825) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Tumor necrosis factor

CHEMBL1825

Anchored from Assay target.

Protein identity Tumor necrosis factor

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

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

Target

Tumor necrosis factor (CHEMBL1825) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Discovery of a Novel Potent and Selective Calcium Release-Activated Calcium Channel Inhibitor: 2,6-Difluoro-<i>N</i>-(2'-methyl-3'-(4-methyl-5-oxo-4,5-dihydro-1,3,4-oxadiazol-2-yl)-[1,1'-biphenyl]-4-yl)benzamide. Structure-Activity Relationship and Preclinical Characterization.

Khedkar NR, Irlapatti NR, Dadke D, Kanoje V, Shaikh Z, Karche V, Shinde V, Deshmukh G, Patil A, Jachak S, Phukan S, Kizhakinagath PA, Gholve M, Bhankhede T, Daler J, Nemade HN, Budhe S, Pareek H, Yeshodharan R, Gupta R, Kalia A, Pandey D, Wagh A, Kumar S, Patil V, Modi D, Sharma N, Ahirrao P, Mehta M, Kumar H, Nigade P, Tamane K, Mallurwar S, Kuldharan S, Pawar S, Vishwase G, Bokan S, Singh M, Naik K, Ingawale S, Shankar R, Kamalakannan P, Venugopal S, George SK, Padiya KJ, Nemmani KVS, Gundu J, Bhonde M, Narasimham L, Sindkhedkar M, Shah C, Sinha N, Sharma S, Bakhle D, Kamboj RK, Palle VP.
J Med Chem (2021) 64 : 17004 -17030
PubMed 34843241 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	6.16	6.16

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL4868242	—	—	1	6.16

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL4868242	—	IC50	=	694.5	nM	6.16