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Assay Detail

CHEMBL4046594

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

ADMET
Inhibition of JAK2 (unknown origin) assessed as reduction in EPO-mediated STAT5 phosphorylation by cell based readout assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Tyrosine-protein kinase JAK2 (CHEMBL2971)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of an imidazopyridine scaffold to generate potent and selective TYK2 inhibitors that demonstrate activity in an in vivo psoriasis model.
Liang J, Van Abbema A, Balazs M, Barrett K, Berezhkovsky L, Blair WS, Chang C, Delarosa D, DeVoss J, Driscoll J, Eigenbrot C, Goodacre S, Ghilardi N, MacLeod C, Johnson A, Bir Kohli P, Lai Y, Lin Z, Mantik P, Menghrajani K, Nguyen H, Peng I, Sambrone A, Shia S, Smith J, Sohn S, Tsui V, Ultsch M, Williams K, Wu LC, Yang W, Zhang B, Magnuson S.
Bioorg Med Chem Lett (2017) 27 : 4370 -4376
PubMed 28830649 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 18 5.79 6.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4093872 1 6.34
CHEMBL4062680 1 6.21
CHEMBL4071399 1 6.19
CHEMBL4097446 1 6.09
CHEMBL4075453 1 6.00
CHEMBL4070262 1 5.96
CHEMBL4080904 1 5.96
CHEMBL4084436 1 5.89
CHEMBL4076947 1 5.85
CHEMBL4092116 1 5.80
CHEMBL4062758 1 5.72
CHEMBL4069942 1 5.68
CHEMBL2387223 1 5.65
CHEMBL4099854 1 5.19
CHEMBL4092191 1 5.11
CHEMBL4105148 1 5.00
CHEMBL4065419 1 -
CHEMBL4093092 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4093872 EC50 = 460.0 nM 6.34
CHEMBL4062680 EC50 = 620.0 nM 6.21
CHEMBL4071399 EC50 = 640.0 nM 6.19
CHEMBL4097446 EC50 = 820.0 nM 6.09
CHEMBL4075453 EC50 = 1000.0 nM 6.00
CHEMBL4070262 EC50 = 1100.0 nM 5.96
CHEMBL4080904 EC50 = 1100.0 nM 5.96
CHEMBL4084436 EC50 = 1300.0 nM 5.89
CHEMBL4076947 EC50 = 1400.0 nM 5.85
CHEMBL4092116 EC50 = 1600.0 nM 5.80
CHEMBL4062758 EC50 = 1900.0 nM 5.72
CHEMBL4069942 EC50 = 2100.0 nM 5.68
CHEMBL2387223 EC50 = 2250.0 nM 5.65
CHEMBL4099854 EC50 = 6500.0 nM 5.19
CHEMBL4092191 EC50 = 7700.0 nM 5.11
CHEMBL4105148 EC50 = 10000.0 nM 5.00
CHEMBL4065419 EC50 - -
CHEMBL4093092 EC50 - -