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Assay Detail

CHEMBL3603330

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Functional
Antiproliferative activity against mouse BA/F3 cells expressing TYK2 E957D mutant after 72 hrs by cell titer glo assay
ChEMBL ↗
64
Total Activities
64
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type BaF3
Confidence 1 — Organism
Curated By Autocuration

Target

NON-PROTEIN TARGET (CHEMBL3879801) ↗
Type NON-MOLECULAR

Publication

Development of Selective Covalent Janus Kinase 3 Inhibitors.
Tan L, Akahane K, McNally R, Reyskens KM, Ficarro SB, Liu S, Herter-Sprie GS, Koyama S, Pattison MJ, Labella K, Johannessen L, Akbay EA, Wong KK, Frank DA, Marto JA, Look TA, Arthur JS, Eck MJ, Gray NS.
J Med Chem (2015) 58 : 6589 -6606
PubMed 26258521 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 64 5.46 6.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3601227 — — 1 6.22
CHEMBL3601706 — — 1 6.12
CHEMBL3601107 — — 1 6.12
CHEMBL3601705 — — 1 6.11
CHEMBL3601228 — — 1 6.06
CHEMBL3601106 — — 1 6.00
CHEMBL3601229 — — 1 6.00
CHEMBL3600393 — — 1 5.96
CHEMBL3601712 — — 1 5.95
CHEMBL3601226 — — 1 5.88
CHEMBL3601230 — — 1 5.88
CHEMBL3601711 — — 1 5.88
CHEMBL3601242 — — 1 5.84
CHEMBL3601232 — — 1 5.81
CHEMBL3601117 — — 1 5.80
CHEMBL3601127 — — 1 5.80
CHEMBL3601716 — — 1 5.74
CHEMBL3601113 — — 1 5.72
CHEMBL3601715 — — 1 5.70
CHEMBL3601114 — — 1 5.65
CHEMBL3601116 — — 1 5.64
CHEMBL3601223 — — 1 5.64
CHEMBL3601231 — — 1 5.63
CHEMBL3601244 — — 1 5.60
CHEMBL3601111 — — 1 5.52
CHEMBL3601718 — — 1 5.50
CHEMBL3601119 — — 1 5.49
CHEMBL3601728 — — 1 5.49
CHEMBL3601725 — — 1 5.48
CHEMBL3601726 — — 1 5.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3601227 — IC50 = 599.0 nM 6.22
CHEMBL3601706 — IC50 = 754.0 nM 6.12
CHEMBL3601107 — IC50 = 759.0 nM 6.12
CHEMBL3601705 — IC50 = 778.0 nM 6.11
CHEMBL3601228 — IC50 = 874.0 nM 6.06
CHEMBL3601106 — IC50 = 994.0 nM 6.00
CHEMBL3601229 — IC50 = 992.0 nM 6.00
CHEMBL3600393 — IC50 = 1099.0 nM 5.96
CHEMBL3601712 — IC50 = 1122.0 nM 5.95
CHEMBL3601226 — IC50 = 1320.0 nM 5.88
CHEMBL3601230 — IC50 = 1318.0 nM 5.88
CHEMBL3601711 — IC50 = 1318.0 nM 5.88
CHEMBL3601242 — IC50 = 1429.0 nM 5.84
CHEMBL3601232 — IC50 = 1542.0 nM 5.81
CHEMBL3601127 — IC50 = 1598.0 nM 5.80
CHEMBL3601117 — IC50 = 1576.0 nM 5.80
CHEMBL3601716 — IC50 = 1836.0 nM 5.74
CHEMBL3601113 — IC50 = 1887.0 nM 5.72
CHEMBL3601715 — IC50 = 2005.0 nM 5.70
CHEMBL3601114 — IC50 = 2227.0 nM 5.65
CHEMBL3601116 — IC50 = 2291.0 nM 5.64
CHEMBL3601223 — IC50 = 2266.0 nM 5.64
CHEMBL3601231 — IC50 = 2353.0 nM 5.63
CHEMBL3601244 — IC50 = 2492.0 nM 5.60
CHEMBL3601111 — IC50 = 3043.0 nM 5.52
CHEMBL3601718 — IC50 = 3163.0 nM 5.50
CHEMBL3601728 — IC50 = 3212.0 nM 5.49
CHEMBL3601119 — IC50 = 3227.0 nM 5.49
CHEMBL3601725 — IC50 = 3327.0 nM 5.48
CHEMBL3601726 — IC50 = 3503.0 nM 5.46
CHEMBL3601120 — IC50 = 3510.0 nM 5.46
CHEMBL3601708 — IC50 = 3549.0 nM 5.45
CHEMBL3601224 — IC50 = 3756.0 nM 5.42
CHEMBL3601713 — IC50 = 3943.0 nM 5.40
CHEMBL3601121 — IC50 = 4090.0 nM 5.39
CHEMBL3601238 — IC50 = 4171.0 nM 5.38
CHEMBL3601709 — IC50 = 4215.0 nM 5.38
CHEMBL3601723 — IC50 = 4458.0 nM 5.35
CHEMBL3601236 — IC50 = 4666.0 nM 5.33
CHEMBL3601237 — IC50 = 4702.0 nM 5.33
CHEMBL3601861 — IC50 = 4950.0 nM 5.30
CHEMBL3601112 — IC50 = 4998.0 nM 5.30
CHEMBL3601710 — IC50 = 5193.0 nM 5.29
CHEMBL3601704 — IC50 = 5452.0 nM 5.26
CHEMBL3601108 — IC50 = 5581.0 nM 5.25
CHEMBL3601727 — IC50 = 5948.0 nM 5.23
CHEMBL3601714 — IC50 = 5874.0 nM 5.23
CHEMBL3601243 — IC50 = 6502.0 nM 5.19
CHEMBL3601233 — IC50 = 6613.0 nM 5.18
CHEMBL3601707 — IC50 = 6857.0 nM 5.16