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Assay Detail

CHEMBL4834060

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

Binding
Inhibition of PHA-stimulated IL2 secretion in human Jurkat T cells preincubated for 10 mins followed by PHA addition and measured after 20 to 24 hrs by ELISA
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Interleukin-2 (CHEMBL5880)
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 24 7.23 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4857063 1 8.10
CHEMBL4868242 1 7.96
CHEMBL4869725 1 7.85
CHEMBL4868367 1 7.50
CHEMBL4848840 1 7.47
CHEMBL4861512 1 7.47
CHEMBL4868517 1 7.30
CHEMBL4859192 1 7.26
CHEMBL4859714 1 7.19
CHEMBL4855379 1 7.19
CHEMBL4854994 1 7.16
CHEMBL4872086 1 7.11
CHEMBL4868543 1 7.03
CHEMBL4848699 1 6.82
CHEMBL4862512 1 6.77
CHEMBL4874097 1 6.75
CHEMBL4872805 1 6.64
CHEMBL4871844 1 6.48
CHEMBL4867119 1 -
CHEMBL4879301 1 -
CHEMBL4868782 1 -
CHEMBL4859561 1 -
CHEMBL4870286 1 -
CHEMBL4864080 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4857063 IC50 = 8.0 nM 8.10
CHEMBL4868242 IC50 = 11.0 nM 7.96
CHEMBL4869725 IC50 = 14.0 nM 7.85
CHEMBL4868367 IC50 = 32.0 nM 7.50
CHEMBL4848840 IC50 = 34.0 nM 7.47
CHEMBL4861512 IC50 = 34.0 nM 7.47
CHEMBL4868517 IC50 = 50.0 nM 7.30
CHEMBL4859192 IC50 = 55.0 nM 7.26
CHEMBL4859714 IC50 = 64.0 nM 7.19
CHEMBL4855379 IC50 = 64.8 nM 7.19
CHEMBL4854994 IC50 = 69.0 nM 7.16
CHEMBL4872086 IC50 = 78.0 nM 7.11
CHEMBL4868543 IC50 = 94.4 nM 7.03
CHEMBL4848699 IC50 = 150.0 nM 6.82
CHEMBL4862512 IC50 = 171.0 nM 6.77
CHEMBL4874097 IC50 = 178.0 nM 6.75
CHEMBL4872805 IC50 = 227.0 nM 6.64
CHEMBL4871844 IC50 = 328.0 nM 6.48
CHEMBL4867119 IC50 - -
CHEMBL4879301 IC50 - -
CHEMBL4868782 IC50 - -
CHEMBL4859561 IC50 - -
CHEMBL4870286 IC50 - -
CHEMBL4864080 IC50 - -