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Assay Detail

CHEMBL4046589

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

Binding
Inhibition of TYK2 (unknown origin) by biochemical assay
32
Total Activities
32
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

Non-receptor tyrosine-protein kinase TYK2 (CHEMBL3553)
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
Ki 32 8.61 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4084436 1 9.52
CHEMBL4062758 1 9.40
CHEMBL4075453 1 9.30
CHEMBL4071399 1 9.30
CHEMBL3675685 1 9.30
CHEMBL4062680 1 9.22
CHEMBL4092116 1 9.22
CHEMBL4093872 1 9.22
CHEMBL4069942 1 9.22
CHEMBL4074130 1 9.22
CHEMBL4076947 1 9.15
CHEMBL4092191 1 9.15
CHEMBL4099854 1 9.15
CHEMBL4093172 1 9.10
CHEMBL4070262 1 9.00
CHEMBL4080904 1 8.92
CHEMBL4097446 1 8.92
CHEMBL4100889 1 8.89
CHEMBL2387223 1 8.80
CHEMBL4064189 1 8.77
CHEMBL4065419 1 8.49
CHEMBL2387224 1 8.32
CHEMBL4105148 1 8.29
CHEMBL4068427 1 8.06
CHEMBL4093092 1 8.00
CHEMBL4075131 1 7.89
CHEMBL4101734 1 7.77
CHEMBL4089568 1 7.72
CHEMBL4085414 1 7.70
CHEMBL4103341 1 7.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4084436 Ki = 0.3 nM 9.52
CHEMBL4062758 Ki = 0.4 nM 9.40
CHEMBL4075453 Ki = 0.5 nM 9.30
CHEMBL4071399 Ki = 0.5 nM 9.30
CHEMBL3675685 Ki = 0.5 nM 9.30
CHEMBL4062680 Ki = 0.6 nM 9.22
CHEMBL4092116 Ki = 0.6 nM 9.22
CHEMBL4093872 Ki = 0.6 nM 9.22
CHEMBL4069942 Ki = 0.6 nM 9.22
CHEMBL4074130 Ki = 0.6 nM 9.22
CHEMBL4076947 Ki = 0.7 nM 9.15
CHEMBL4092191 Ki = 0.7 nM 9.15
CHEMBL4099854 Ki = 0.7 nM 9.15
CHEMBL4093172 Ki = 0.8 nM 9.10
CHEMBL4070262 Ki = 1.0 nM 9.00
CHEMBL4097446 Ki = 1.2 nM 8.92
CHEMBL4080904 Ki = 1.2 nM 8.92
CHEMBL4100889 Ki = 1.3 nM 8.89
CHEMBL2387223 Ki = 1.6 nM 8.80
CHEMBL4064189 Ki = 1.7 nM 8.77
CHEMBL4065419 Ki = 3.2 nM 8.49
CHEMBL2387224 Ki = 4.8 nM 8.32
CHEMBL4105148 Ki = 5.1 nM 8.29
CHEMBL4068427 Ki = 8.8 nM 8.06
CHEMBL4093092 Ki = 9.9 nM 8.00
CHEMBL4075131 Ki = 13.0 nM 7.89
CHEMBL4101734 Ki = 17.0 nM 7.77
CHEMBL4089568 Ki = 19.0 nM 7.72
CHEMBL4085414 Ki = 20.0 nM 7.70
CHEMBL4103341 Ki = 31.0 nM 7.51
CHEMBL4082575 Ki = 42.0 nM 7.38
CHEMBL4086518 Ki = 3500.0 nM 5.46