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Assay Detail

CHEMBL4833083

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

Binding
Inverse agonist activity at human RORC2 assessed as inhibition of SRC1-derived coactivator peptide by TR-FRET assay
ChEMBL ↗
46
Total Activities
46
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

Nuclear receptor ROR-gamma (CHEMBL1741186) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

AZD0284, a Potent, Selective, and Orally Bioavailable Inverse Agonist of Retinoic Acid Receptor-Related Orphan Receptor C2.
Narjes F, Llinas A, von Berg S, Jirholt J, Lever S, Pehrson R, Collins M, Malmberg A, Svanberg P, Xue Y, Olsson RI, Malmberg J, Hughes G, Hossain N, Grindebacke H, Leffler A, Krutrök N, Bäck E, Ramnegård M, Lepistö M, Thunberg L, Aagaard A, McPheat J, Hansson EL, Chen R, Xiong Y, Hansson TG.
J Med Chem (2021) 64 : 13807 -13829
PubMed 34464130 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 46 7.04 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4857395 — — 1 7.52
CHEMBL4866908 — — 1 7.42
CHEMBL4862137 — — 1 7.41
CHEMBL4864731 — — 1 7.39
CHEMBL4857284 — — 1 7.39
CHEMBL4864604 — — 1 7.39
CHEMBL4869175 — — 1 7.33
CHEMBL4463668 — — 1 7.32
CHEMBL4849302 — — 1 7.32
CHEMBL4856950 — — 1 7.31
CHEMBL4868864 — — 1 7.30
CHEMBL4864990 — — 1 7.29
CHEMBL4855387 — — 1 7.29
CHEMBL4877500 — — 1 7.23
CHEMBL4866227 — — 1 7.23
CHEMBL4847134 — — 1 7.23
CHEMBL4846059 — — 1 7.22
CHEMBL4852181 — — 1 7.20
CHEMBL4878173 — — 1 7.19
CHEMBL4845714 — — 1 7.19
CHEMBL4855766 — — 1 7.19
CHEMBL4856430 — — 1 7.19
CHEMBL4865776 — — 1 7.19
CHEMBL4865352 — — 1 7.19
CHEMBL4854122 — — 1 7.17
CHEMBL4847308 — — 1 7.17
CHEMBL4850359 — — 1 7.10
CHEMBL4870339 — — 1 7.10
CHEMBL4872141 — — 1 7.08
CHEMBL4848388 — — 1 7.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4857395 — IC50 = 30.0 nM 7.52
CHEMBL4866908 — IC50 = 38.0 nM 7.42
CHEMBL4862137 — IC50 = 39.0 nM 7.41
CHEMBL4864731 — IC50 = 41.0 nM 7.39
CHEMBL4857284 — IC50 = 41.0 nM 7.39
CHEMBL4864604 — IC50 = 41.0 nM 7.39
CHEMBL4869175 — IC50 = 47.0 nM 7.33
CHEMBL4463668 — IC50 = 48.0 nM 7.32
CHEMBL4849302 — IC50 = 48.0 nM 7.32
CHEMBL4856950 — IC50 = 49.0 nM 7.31
CHEMBL4868864 — IC50 = 50.0 nM 7.30
CHEMBL4864990 — IC50 = 51.0 nM 7.29
CHEMBL4855387 — IC50 = 51.0 nM 7.29
CHEMBL4847134 — IC50 = 59.0 nM 7.23
CHEMBL4866227 — IC50 = 59.0 nM 7.23
CHEMBL4877500 — IC50 = 59.0 nM 7.23
CHEMBL4846059 — IC50 = 60.0 nM 7.22
CHEMBL4852181 — IC50 = 63.0 nM 7.20
CHEMBL4865352 — IC50 = 64.0 nM 7.19
CHEMBL4865776 — IC50 = 64.0 nM 7.19
CHEMBL4856430 — IC50 = 65.0 nM 7.19
CHEMBL4845714 — IC50 = 65.0 nM 7.19
CHEMBL4878173 — IC50 = 64.0 nM 7.19
CHEMBL4855766 — IC50 = 65.0 nM 7.19
CHEMBL4854122 — IC50 = 67.0 nM 7.17
CHEMBL4847308 — IC50 = 67.0 nM 7.17
CHEMBL4850359 — IC50 = 79.0 nM 7.10
CHEMBL4870339 — IC50 = 80.0 nM 7.10
CHEMBL4872141 — IC50 = 83.0 nM 7.08
CHEMBL4848388 — IC50 = 88.0 nM 7.06
CHEMBL4853746 — IC50 = 93.0 nM 7.03
CHEMBL4856963 — IC50 = 96.0 nM 7.02
CHEMBL4852138 — IC50 = 97.0 nM 7.01
CHEMBL4875667 — IC50 = 106.0 nM 6.97
CHEMBL4847761 — IC50 = 121.0 nM 6.92
CHEMBL4875795 — IC50 = 128.0 nM 6.89
CHEMBL4859385 — IC50 = 134.0 nM 6.87
CHEMBL4876902 — IC50 = 134.0 nM 6.87
CHEMBL4868403 — IC50 = 146.0 nM 6.84
CHEMBL4865573 — IC50 = 161.0 nM 6.79
CHEMBL4853971 — IC50 = 190.0 nM 6.72
CHEMBL4870856 — IC50 = 194.0 nM 6.71
CHEMBL4870686 — IC50 = 195.0 nM 6.71
CHEMBL4875842 — IC50 = 326.0 nM 6.49
CHEMBL4850055 — IC50 = 2044.0 nM 5.69
CHEMBL4868767 — IC50 = 16921.0 nM 4.77