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Assay Detail

CHEMBL977319

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

Binding
Displacement of [3H]PDBu from RasGRP3 expressed in cells
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Ras guanyl-releasing protein 3 (CHEMBL3638)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Conformationally constrained analogues of diacylglycerol. 30. An investigation of diacylglycerol-lactones containing heteroaryl groups reveals compounds with high selectivity for Ras guanyl nucleotide-releasing proteins.
El Kazzouli S, Lewin NE, Blumberg PM, Marquez VE.
J Med Chem (2008) 51 : 5371 -5386
PubMed 18707088 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 36 7.45 9.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL519741 1 9.74
CHEMBL530110 1 9.70
CHEMBL488872 1 9.28
CHEMBL488667 1 9.15
CHEMBL472007 1 9.14
CHEMBL472522 1 8.80
CHEMBL529000 1 8.77
CHEMBL488674 1 8.48
CHEMBL472521 1 8.43
CHEMBL488675 1 8.42
CHEMBL488871 1 8.34
CHEMBL488668 1 8.17
CHEMBL487473 1 8.09
CHEMBL511472 1 7.96
CHEMBL472523 1 7.86
CHEMBL488509 1 7.76
CHEMBL487483 1 7.62
CHEMBL488707 1 7.49
CHEMBL470094 1 7.45
CHEMBL443643 1 7.36
CHEMBL487822 1 7.27
CHEMBL488670 1 7.27
CHEMBL487484 1 7.23
CHEMBL471316 1 7.09
CHEMBL512538 1 7.08
CHEMBL472183 1 6.86
CHEMBL511847 1 6.17
CHEMBL528323 1 6.04
CHEMBL530337 1 5.86
CHEMBL472351 1 5.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL519741 Ki = 0.18 nM 9.74
CHEMBL530110 Ki = 0.2 nM 9.70
CHEMBL488872 Ki = 0.52 nM 9.28
CHEMBL488667 Ki = 0.7 nM 9.15
CHEMBL472007 Ki = 0.72 nM 9.14
CHEMBL472522 Ki = 1.6 nM 8.80
CHEMBL529000 Ki = 1.7 nM 8.77
CHEMBL488674 Ki = 3.3 nM 8.48
CHEMBL472521 Ki = 3.7 nM 8.43
CHEMBL488675 Ki = 3.8 nM 8.42
CHEMBL488871 Ki = 4.6 nM 8.34
CHEMBL488668 Ki = 6.7 nM 8.17
CHEMBL487473 Ki = 8.2 nM 8.09
CHEMBL511472 Ki = 11.0 nM 7.96
CHEMBL472523 Ki = 13.8 nM 7.86
CHEMBL488509 Ki = 17.4 nM 7.76
CHEMBL487483 Ki = 23.8 nM 7.62
CHEMBL488707 Ki = 32.2 nM 7.49
CHEMBL470094 Ki = 35.8 nM 7.45
CHEMBL443643 Ki = 44.0 nM 7.36
CHEMBL487822 Ki = 54.2 nM 7.27
CHEMBL488670 Ki = 54.0 nM 7.27
CHEMBL487484 Ki = 59.0 nM 7.23
CHEMBL471316 Ki = 81.0 nM 7.09
CHEMBL512538 Ki = 83.0 nM 7.08
CHEMBL472183 Ki = 137.0 nM 6.86
CHEMBL511847 Ki = 670.0 nM 6.17
CHEMBL528323 Ki = 907.0 nM 6.04
CHEMBL530337 Ki = 1390.0 nM 5.86
CHEMBL472351 Ki = 1410.0 nM 5.85
CHEMBL488506 Ki = 1970.0 nM 5.71
CHEMBL471142 Ki = 2040.0 nM 5.69
CHEMBL488671 Ki = 2360.0 nM 5.63
CHEMBL513379 Ki = 2470.0 nM 5.61
CHEMBL486457 Ki = 3660.0 nM 5.44
CHEMBL472006 Ki = 5500.0 nM 5.26