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Assay Detail

CHEMBL3106087

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

Binding
Inhibition of APC-labeled RORgammat receptor ligand binding domain (unknown origin) after 1 hr by FRET assay
ChEMBL ↗
52
Total Activities
52
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

Discovery of novel N-(5-(arylcarbonyl)thiazol-2-yl)amides and N-(5-(arylcarbonyl)thiophen-2-yl)amides as potent RORγt inhibitors.
Wang Y, Cai W, Zhang G, Yang T, Liu Q, Cheng Y, Zhou L, Ma Y, Cheng Z, Lu S, Zhao YG, Zhang W, Xiang Z, Wang S, Yang L, Wu Q, Orband-Miller LA, Xu Y, Zhang J, Gao R, Huxdorf M, Xiang JN, Zhong Z, Elliott JD, Leung S, Lin X.
Bioorg Med Chem (2014) 22 : 692 -702
PubMed 24388993 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 52 6.46 8.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3105670 — — 1 8.20
CHEMBL3105669 — — 1 8.10
CHEMBL3105692 — — 1 8.00
CHEMBL3105672 — — 1 8.00
CHEMBL3105682 — — 1 8.00
CHEMBL3105686 — — 1 8.00
CHEMBL3105671 — — 1 7.90
CHEMBL3105676 — — 1 7.90
CHEMBL3105683 — — 1 7.90
CHEMBL3105690 — — 1 7.90
CHEMBL3105681 — — 1 7.80
CHEMBL3105691 — — 1 7.80
CHEMBL3105684 — — 1 7.70
CHEMBL3105685 — — 1 7.60
CHEMBL3105673 — — 1 7.60
CHEMBL3105674 — — 1 7.50
CHEMBL3105678 — — 1 7.50
CHEMBL3105677 — — 1 7.40
CHEMBL3105675 — — 1 7.40
CHEMBL3102888 — — 1 6.40
CHEMBL3105804 — — 1 6.20
CHEMBL3105679 — — 1 6.10
CHEMBL3105798 — — 1 6.10
CHEMBL3105815 — — 1 6.00
CHEMBL3105819 — — 1 5.90
CHEMBL3105799 — — 1 5.90
CHEMBL3105816 — — 1 5.80
CHEMBL3105695 — — 1 5.80
CHEMBL3105803 — — 1 5.70
CHEMBL3105795 — — 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3105670 — IC50 = 6.31 nM 8.20
CHEMBL3105669 — IC50 = 7.943 nM 8.10
CHEMBL3105672 — IC50 = 10.0 nM 8.00
CHEMBL3105682 — IC50 = 10.0 nM 8.00
CHEMBL3105686 — IC50 = 10.0 nM 8.00
CHEMBL3105692 — IC50 = 10.0 nM 8.00
CHEMBL3105671 — IC50 = 12.59 nM 7.90
CHEMBL3105676 — IC50 = 12.59 nM 7.90
CHEMBL3105683 — IC50 = 12.59 nM 7.90
CHEMBL3105690 — IC50 = 12.59 nM 7.90
CHEMBL3105681 — IC50 = 15.85 nM 7.80
CHEMBL3105691 — IC50 = 15.85 nM 7.80
CHEMBL3105684 — IC50 = 19.95 nM 7.70
CHEMBL3105685 — IC50 = 25.12 nM 7.60
CHEMBL3105673 — IC50 = 25.12 nM 7.60
CHEMBL3105674 — IC50 = 31.62 nM 7.50
CHEMBL3105678 — IC50 = 31.62 nM 7.50
CHEMBL3105677 — IC50 = 39.81 nM 7.40
CHEMBL3105675 — IC50 = 39.81 nM 7.40
CHEMBL3102888 — IC50 = 398.11 nM 6.40
CHEMBL3105804 — IC50 = 630.96 nM 6.20
CHEMBL3105679 — IC50 = 794.33 nM 6.10
CHEMBL3105798 — IC50 = 794.33 nM 6.10
CHEMBL3105815 — IC50 = 1000.0 nM 6.00
CHEMBL3105799 — IC50 = 1258.93 nM 5.90
CHEMBL3105819 — IC50 = 1258.93 nM 5.90
CHEMBL3105816 — IC50 = 1584.89 nM 5.80
CHEMBL3105695 — IC50 = 1584.89 nM 5.80
CHEMBL3105803 — IC50 = 1995.26 nM 5.70
CHEMBL3105795 — IC50 = 1995.26 nM 5.70
CHEMBL3105807 — IC50 = 2511.89 nM 5.60
CHEMBL3105797 — IC50 = 3981.07 nM 5.40
CHEMBL3105796 — IC50 = 3981.07 nM 5.40
CHEMBL3105814 — IC50 = 3981.07 nM 5.40
CHEMBL3105802 — IC50 = 5011.87 nM 5.30
CHEMBL3105813 — IC50 = 5011.87 nM 5.30
CHEMBL3105817 — IC50 = 5011.87 nM 5.30
CHEMBL3105800 — IC50 = 6309.57 nM 5.20
CHEMBL3105806 — IC50 = 6309.57 nM 5.20
CHEMBL3105794 — IC50 = 7943.28 nM 5.10
CHEMBL3105812 — IC50 = 7943.28 nM 5.10
CHEMBL3105680 — IC50 = 7943.28 nM 5.10
CHEMBL3105801 — IC50 = 10000.0 nM 5.00
CHEMBL3105811 — IC50 = 10000.0 nM 5.00
CHEMBL3105805 — IC50 = 10000.0 nM 5.00
CHEMBL3105820 — IC50 = 12589.25 nM 4.90
CHEMBL3105810 — IC50 > 25118.86 nM -
CHEMBL3105809 — IC50 > 25118.86 nM -
CHEMBL3105808 — IC50 > 25118.86 nM -
CHEMBL3105818 — IC50 > 25118.86 nM -