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Assay Detail

CHEMBL1833078

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

Binding
Displacement of [3H]PK11195 from TSPO receptor in rat kidney membranes
ChEMBL ↗
53
Total Activities
53
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Translocator protein (CHEMBL4552) ↗
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Tertiary amides with a five-membered heteroaromatic ring as new probes for the translocator protein.
Cosimelli B, Simorini F, Taliani S, La Motta C, Da Settimo F, Severi E, Greco G, Novellino E, Costa B, Da Pozzo E, Bendinelli S, Martini C.
Eur J Med Chem (2011) 46 : 4506 -4520
PubMed 21824692 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 53 6.29 8.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL481537 PK-11195 — 1 8.03
CHEMBL1830760 — — 1 7.96
CHEMBL286346 RO-54864 — 1 7.64
CHEMBL1830752 — — 1 7.50
CHEMBL1830756 — — 1 7.35
CHEMBL1830767 — — 1 7.29
CHEMBL1830764 — — 1 7.17
CHEMBL1830759 — — 1 7.06
CHEMBL1830744 — — 1 6.88
CHEMBL1830748 — — 1 6.82
CHEMBL1830753 — — 1 6.82
CHEMBL1830761 — — 1 6.80
CHEMBL1830755 — — 1 6.75
CHEMBL1830766 — — 1 6.59
CHEMBL1830747 — — 1 6.57
CHEMBL1830751 — — 1 6.46
CHEMBL1830738 — — 1 6.42
CHEMBL1830733 — — 1 6.42
CHEMBL1830743 — — 1 6.31
CHEMBL1830763 — — 1 6.31
CHEMBL1830727 — — 1 6.21
CHEMBL1830737 — — 1 6.21
CHEMBL1830732 — — 1 6.19
CHEMBL1830757 — — 1 6.15
CHEMBL1830719 — — 1 6.11
CHEMBL1830765 — — 1 6.06
CHEMBL1830720 — — 1 6.04
CHEMBL1830754 — — 1 6.03
CHEMBL1830745 — — 1 5.96
CHEMBL1830758 — — 1 5.79

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL481537 PK-11195 Ki = 9.3 nM 8.03
CHEMBL1830760 — Ki = 11.0 nM 7.96
CHEMBL286346 RO-54864 Ki = 23.0 nM 7.64
CHEMBL1830752 — Ki = 32.0 nM 7.50
CHEMBL1830756 — Ki = 45.0 nM 7.35
CHEMBL1830767 — Ki = 51.0 nM 7.29
CHEMBL1830764 — Ki = 68.0 nM 7.17
CHEMBL1830759 — Ki = 88.0 nM 7.06
CHEMBL1830744 — Ki = 133.0 nM 6.88
CHEMBL1830748 — Ki = 152.0 nM 6.82
CHEMBL1830753 — Ki = 151.0 nM 6.82
CHEMBL1830761 — Ki = 157.0 nM 6.80
CHEMBL1830755 — Ki = 177.0 nM 6.75
CHEMBL1830766 — Ki = 257.0 nM 6.59
CHEMBL1830747 — Ki = 267.0 nM 6.57
CHEMBL1830751 — Ki = 346.0 nM 6.46
CHEMBL1830738 — Ki = 382.0 nM 6.42
CHEMBL1830733 — Ki = 379.0 nM 6.42
CHEMBL1830743 — Ki = 489.0 nM 6.31
CHEMBL1830763 — Ki = 487.0 nM 6.31
CHEMBL1830727 — Ki = 613.0 nM 6.21
CHEMBL1830737 — Ki = 620.0 nM 6.21
CHEMBL1830732 — Ki = 651.0 nM 6.19
CHEMBL1830757 — Ki = 704.0 nM 6.15
CHEMBL1830719 — Ki = 772.0 nM 6.11
CHEMBL1830765 — Ki = 877.0 nM 6.06
CHEMBL1830720 — Ki = 914.0 nM 6.04
CHEMBL1830754 — Ki = 942.0 nM 6.03
CHEMBL1830745 — Ki = 1100.0 nM 5.96
CHEMBL1830758 — Ki = 1630.0 nM 5.79
CHEMBL1830750 — Ki = 1698.0 nM 5.77
CHEMBL1830762 — Ki = 2200.0 nM 5.66
CHEMBL1830735 — Ki = 2700.0 nM 5.57
CHEMBL1830749 — Ki = 3200.0 nM 5.50
CHEMBL1830746 — Ki = 3400.0 nM 5.47
CHEMBL1830726 — Ki = 3462.0 nM 5.46
CHEMBL1830721 — Ki = 4193.0 nM 5.38
CHEMBL1830742 — Ki = 4340.0 nM 5.36
CHEMBL1830728 — Ki = 4601.0 nM 5.34
CHEMBL1830722 — Ki = 4873.0 nM 5.31
CHEMBL1830729 — Ki = 5487.0 nM 5.26
CHEMBL1830739 — Ki = 5800.0 nM 5.24
CHEMBL1830734 — Ki = 7000.0 nM 5.16
CHEMBL1830730 — Ki > 10000.0 nM -
CHEMBL1830725 — Ki > 10000.0 nM -
CHEMBL1830724 — Ki > 10000.0 nM -
CHEMBL1830723 — Ki > 10000.0 nM -
CHEMBL1830731 — Ki > 10000.0 nM -
CHEMBL1830740 — Ki > 10000.0 nM -
CHEMBL1830741 — Ki > 10000.0 nM -