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Assay Detail

CHEMBL4620707

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Binding
Inverse agonist activity at RORgammat in human whole blood assessed as inhibition of anti-CD3/anti-CD28 monoclonal antibodies-stimulated IL-17A production measured after 3 days by ELISA
ChEMBL ↗
48
Total Activities
48
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Tissue Blood
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Optimization and biological evaluation of thiazole-bis-amide inverse agonists of RORγt.
Gege C, Albers M, Kinzel O, Kleymann G, Schlüter T, Steeneck C, Hoffmann T, Xue X, Cummings MD, Spurlino J, Milligan C, Fourie AM, Edwards JP, Leonard K, Coe K, Scott B, Pippel D, Goldberg SD.
Bioorg Med Chem Lett (2020) 30 : 127205 -127205
PubMed 32336498 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 46 6.59 7.51
IC50 2 6.40 6.65

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4646215 — — 1 7.51
CHEMBL4644553 — — 1 7.43
CHEMBL4635866 — — 1 7.17
CHEMBL4643698 — — 1 7.08
CHEMBL4646118 — — 1 7.01
CHEMBL4640811 — — 1 7.00
CHEMBL4643996 — — 1 6.96
CHEMBL4635066 — — 1 6.93
CHEMBL4643780 — — 1 6.91
CHEMBL4636470 — — 1 6.86
CHEMBL4637518 — — 1 6.84
CHEMBL4639646 — — 1 6.83
CHEMBL4634281 — — 1 6.83
CHEMBL4644115 — — 1 6.82
CHEMBL4648715 — — 1 6.82
CHEMBL4642426 — — 1 6.80
CHEMBL4639653 — — 1 6.80
CHEMBL4645439 — — 1 6.78
CHEMBL4634571 — — 1 6.76
CHEMBL4644560 — — 1 6.75
CHEMBL4639401 — — 1 6.73
CHEMBL4645069 — — 1 6.72
CHEMBL4649882 — — 1 6.70
CHEMBL4129202 — — 1 6.65
CHEMBL4636603 — — 1 6.57
CHEMBL4646799 — — 1 6.51
CHEMBL4648138 — — 1 6.48
CHEMBL4645916 — — 1 6.47
CHEMBL4647147 — — 1 6.45
CHEMBL4639213 — — 1 6.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4646215 — EC50 = 31.0 nM 7.51
CHEMBL4644553 — EC50 = 37.0 nM 7.43
CHEMBL4635866 — EC50 = 68.0 nM 7.17
CHEMBL4643698 — EC50 = 83.0 nM 7.08
CHEMBL4646118 — EC50 = 98.0 nM 7.01
CHEMBL4640811 — EC50 = 99.0 nM 7.00
CHEMBL4643996 — EC50 = 109.0 nM 6.96
CHEMBL4635066 — EC50 = 118.0 nM 6.93
CHEMBL4643780 — EC50 = 123.0 nM 6.91
CHEMBL4636470 — EC50 = 139.0 nM 6.86
CHEMBL4637518 — EC50 = 146.0 nM 6.84
CHEMBL4639646 — EC50 = 147.0 nM 6.83
CHEMBL4634281 — EC50 = 148.0 nM 6.83
CHEMBL4644115 — EC50 = 150.0 nM 6.82
CHEMBL4648715 — EC50 = 150.0 nM 6.82
CHEMBL4642426 — EC50 = 160.0 nM 6.80
CHEMBL4639653 — EC50 = 157.0 nM 6.80
CHEMBL4645439 — EC50 = 168.0 nM 6.78
CHEMBL4634571 — EC50 = 175.0 nM 6.76
CHEMBL4644560 — EC50 = 177.0 nM 6.75
CHEMBL4639401 — EC50 = 187.0 nM 6.73
CHEMBL4645069 — EC50 = 189.0 nM 6.72
CHEMBL4649882 — EC50 = 201.0 nM 6.70
CHEMBL4129202 — IC50 = 222.0 nM 6.65
CHEMBL4636603 — EC50 = 269.0 nM 6.57
CHEMBL4646799 — EC50 = 308.0 nM 6.51
CHEMBL4648138 — EC50 = 334.0 nM 6.48
CHEMBL4645916 — EC50 = 340.0 nM 6.47
CHEMBL4647147 — EC50 = 353.0 nM 6.45
CHEMBL4639213 — EC50 = 372.0 nM 6.43
CHEMBL4646545 — EC50 = 389.0 nM 6.41
CHEMBL4643849 — EC50 = 397.0 nM 6.40
CHEMBL4643735 — EC50 = 489.0 nM 6.31
CHEMBL4646821 — EC50 = 495.0 nM 6.30
CHEMBL4647352 — EC50 = 497.0 nM 6.30
CHEMBL4644848 — EC50 = 526.0 nM 6.28
CHEMBL4648158 — EC50 = 566.0 nM 6.25
CHEMBL4639405 — EC50 = 587.0 nM 6.23
CHEMBL4645155 — EC50 = 621.0 nM 6.21
CHEMBL4638627 — IC50 = 708.0 nM 6.15
CHEMBL4647081 — EC50 = 721.0 nM 6.14
CHEMBL4633497 — EC50 = 780.0 nM 6.11
CHEMBL4643697 — EC50 = 777.0 nM 6.11
CHEMBL4644817 — EC50 = 794.0 nM 6.10
CHEMBL4649396 — EC50 = 879.0 nM 6.06
CHEMBL4636509 — EC50 = 896.0 nM 6.05
CHEMBL4649516 — EC50 = 917.0 nM 6.04
CHEMBL4648441 — EC50 = 901.0 nM 6.04