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Assay Detail

CHEMBL3375302

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

Binding
Displacement of [3H]25-hydroxycholesterol from human RORc-LBD expressed in bacterial expression system after 3 hrs by scintillation counting analysis
ChEMBL ↗
46
Total Activities
46
Compounds Tested
3
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

A reversed sulfonamide series of selective RORc inverse agonists.
van Niel MB, Fauber BP, Cartwright M, Gaines S, Killen JC, René O, Ward SI, de Leon Boenig G, Deng Y, Eidenschenk C, Everett C, Gancia E, Ganguli A, Gobbi A, Hawkins J, Johnson AR, Kiefer JR, La H, Lockey P, Norman M, Ouyang W, Qin A, Wakes N, Waszkowycz B, Wong H.
Bioorg Med Chem Lett (2014) 24 : 5769 -5776
PubMed 25453817 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 42 7.23 8.22
EC50 3 7.70 7.70
Kd 1 6.96 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3361052 — — 1 8.22
CHEMBL3361050 — — 1 8.22
CHEMBL3361053 — — 1 8.15
CHEMBL3361057 — — 1 8.10
CHEMBL3361049 — — 1 8.04
CHEMBL3361054 — — 1 7.96
CHEMBL3361064 — — 1 7.92
CHEMBL3361055 — — 1 7.85
CHEMBL3361060 — — 1 7.85
CHEMBL3361061 — — 1 7.82
CHEMBL3361058 — — 1 7.80
CHEMBL169046 — — 1 7.70
CHEMBL422904 22(R)-HYDROXYCHOLESTEROL — 1 7.70
CHEMBL1233249 — — 1 7.70
CHEMBL3361059 — — 1 7.68
CHEMBL3361045 — — 1 7.68
CHEMBL3263710 — — 1 7.50
CHEMBL3361051 — — 1 7.48
CHEMBL3263716 — — 1 7.48
CHEMBL3361048 — — 1 7.47
CHEMBL3361027 — — 1 7.43
CHEMBL3361040 — — 1 7.39
CHEMBL3361039 — — 1 7.38
CHEMBL3361038 — — 1 7.29
CHEMBL3361036 — — 1 7.29
CHEMBL3361056 — — 1 7.25
CHEMBL3361047 — — 1 7.21
CHEMBL3361028 — — 1 7.18
CHEMBL3361046 — — 1 7.16
CHEMBL3361037 — — 1 7.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3361052 — IC50 = 6.0 nM 8.22
CHEMBL3361050 — IC50 = 6.0 nM 8.22
CHEMBL3361053 — IC50 = 7.0 nM 8.15
CHEMBL3361057 — IC50 = 8.0 nM 8.10
CHEMBL3361049 — IC50 = 9.2 nM 8.04
CHEMBL3361054 — IC50 = 11.0 nM 7.96
CHEMBL3361064 — IC50 = 12.0 nM 7.92
CHEMBL3361055 — IC50 = 14.0 nM 7.85
CHEMBL3361060 — IC50 = 14.0 nM 7.85
CHEMBL3361061 — IC50 = 15.0 nM 7.82
CHEMBL3361058 — IC50 = 16.0 nM 7.80
CHEMBL1233249 — EC50 = 20.0 nM 7.70
CHEMBL422904 22(R)-HYDROXYCHOLESTEROL EC50 = 20.0 nM 7.70
CHEMBL169046 — EC50 = 20.0 nM 7.70
CHEMBL3361045 — IC50 = 21.0 nM 7.68
CHEMBL3361059 — IC50 = 21.0 nM 7.68
CHEMBL3263710 — IC50 = 32.0 nM 7.50
CHEMBL3361051 — IC50 = 33.0 nM 7.48
CHEMBL3263716 — IC50 = 33.0 nM 7.48
CHEMBL3361048 — IC50 = 34.0 nM 7.47
CHEMBL3361027 — IC50 = 37.0 nM 7.43
CHEMBL3361040 — IC50 = 41.0 nM 7.39
CHEMBL3361039 — IC50 = 42.0 nM 7.38
CHEMBL3361038 — IC50 = 51.0 nM 7.29
CHEMBL3361036 — IC50 = 51.0 nM 7.29
CHEMBL3361056 — IC50 = 56.0 nM 7.25
CHEMBL3361047 — IC50 = 61.0 nM 7.21
CHEMBL3361028 — IC50 = 66.0 nM 7.18
CHEMBL3361046 — IC50 = 70.0 nM 7.16
CHEMBL3361037 — IC50 = 93.0 nM 7.03
CHEMBL1751 DIGOXIN Kd = 109.0 nM 6.96
CHEMBL3263696 — IC50 = 130.0 nM 6.89
CHEMBL3361044 — IC50 = 160.0 nM 6.80
CHEMBL3361029 — IC50 = 160.0 nM 6.80
CHEMBL3361034 — IC50 = 170.0 nM 6.77
CHEMBL3361062 — IC50 = 170.0 nM 6.77
CHEMBL3361063 — IC50 = 180.0 nM 6.75
CHEMBL3361065 — IC50 = 180.0 nM 6.75
CHEMBL3361042 — IC50 = 190.0 nM 6.72
CHEMBL3361043 — IC50 = 340.0 nM 6.47
CHEMBL3361035 — IC50 = 370.0 nM 6.43
CHEMBL3361033 — IC50 = 420.0 nM 6.38
CHEMBL3361041 — IC50 = 430.0 nM 6.37
CHEMBL3361031 — IC50 = 440.0 nM 6.36
CHEMBL3361030 — IC50 = 510.0 nM 6.29
CHEMBL3361032 — IC50 = 5600.0 nM 5.25