Compound Detail

CHEMBL439883

SAUVAGINE

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ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID	CHEMBL439883
Name	SAUVAGINE
Phase	Preclinical
Structure Type	BOTH
InChI Key	KFUIXDNQSMKKJQ-ZLFMSJRASA-N

Targets

Activities

Assay Types

PK Parameters

Publications

Known Names

Molecular Properties

4600.4

MW (Da)

Drug Information

Molecule Type	Protein
Availability	Unknown
Chirality	Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula	C202H345N55O64S
MW	4600.37

Activity Summary

IC50 4 meas. best 9.24

EC50 2 meas. best 7.75

Ki 2 meas. best 9.1

Target Activity Profile

Target	Type	Best pChEMBL	Mean pChEMBL	Best (nM)	# Data
Corticotropin releasing hormone receptor 2 CHEMBL5634	IC50	9.24	9.24	0.6	1
Unchecked CHEMBL612545	IC50	9.24	9.24	0.6	1
Corticotropin-releasing factor receptor 1 CHEMBL1800	Ki	9.1	9.1	0.8	2
Corticotropin-releasing factor receptor 1 CHEMBL1800	IC50	9.05	9.05	0.9	1
Corticotropin-releasing factor receptor 2 CHEMBL4069	IC50	8.8	8.8	1.6	1
Corticotropin-releasing factor receptor 1 CHEMBL2446	EC50	7.75	7.75	17.6	1
Corticotropin-releasing factor receptor 2 CHEMBL2253	EC50	7.22	7.22	60.0	1

Activity Data Samples

Top measurements by pChEMBL value

Target	Type	Rel.	Value	Units	pChEMBL	Assay	PubMed
Corticotropin releasing hormone receptor 2	IC50	=	0.58	nM	9.24	Displacement of [125I]sauvagine from CRF2 receptor in pig choroid plexus by rapi...	19552436
Unchecked	IC50	=	0.58	nM	9.24	Displacement of [125I]sauvagine from CRF2 receptor in porcine choroid plexus hom...	19954247
Corticotropin-releasing factor receptor 1	Ki	=	0.8	nM	9.1	Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK2...	26456805
Corticotropin-releasing factor receptor 1	Ki	=	0.8	nM	9.1	Displacement of [125I]-Tyr0-sauvagine from CRF1 receptor (unknown origin)	26456805
Corticotropin-releasing factor receptor 1	IC50	=	0.9	nM	9.05	Inhibition of recombinant corticotropin releasing factor receptor 1 assayed usin...	12361401
Corticotropin-releasing factor receptor 2	IC50	=	1.6	nM	8.8	Inhibition of recombinant human corticotropin releasing factor receptor 2 beta (...	12361401
Corticotropin-releasing factor receptor 1	EC50	=	17.6	nM	7.75	In vitro effective concentration for mouse corticotropin releasing factor 1 rece...	15634020
Corticotropin-releasing factor receptor 2	EC50	=	60.0	nM	7.22	In vitro effective concentration for mouse corticotropin releasing factor 2 rece...	15634020

Literature References

PubMed	DOI	Target Context	# Activities
15634020	10.1021/jm049490m	Mus musculus	3
15634020	10.1021/jm049490m	Corticotropin-releasing factor receptor 2	2
15634020	10.1021/jm049490m	Corticotropin-releasing factor receptor 1	2
26456805	10.1016/j.bmcl.2015.10.010	Corticotropin-releasing factor receptor 1	2
12361401	10.1021/jm0202122	Corticotropin-releasing factor receptor 1	1
12361401	10.1021/jm0202122	Corticotropin-releasing factor receptor 2	1
19552436	10.1021/jm900302q	Corticotropin releasing hormone receptor 2	1
19954247	10.1021/jm900716v	Unchecked	1
26456805	10.1016/j.bmcl.2015.10.010	Corticotropin-releasing factor receptor 2	1

Data from ChEMBL 36 via Core Engine