DiscoveRx KINOMEscan® screen
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform. http://www.discoverx.com/services/drug-discovery-development-services/kinase-profiling/kinomescan Reference: 1-2
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Target used in screen: KIT
Ligand Sp. Type Action Value (-log10) Parameter Value (nM) Parameter sunitinib Hs Inhibitor Inhibition 9.4 pKd 0.4 Kd cediranib Hs Inhibitor Inhibition 9.4 pKd 0.4 Kd SU-14813 Hs Inhibitor Inhibition 9.2 pKd 0.7 Kd Ki-20227 Hs Inhibitor Inhibition 9.2 pKd 0.7 Kd dasatinib Hs Inhibitor Inhibition 9.1 pKd 0.8 Kd PD-173955 Hs Inhibitor Inhibition 8.7 pKd 1.8 Kd linifanib Hs Inhibitor Inhibition 8.7 pKd 2.0 Kd foretinib Hs Inhibitor Inhibition 8.6 pKd 2.5 Kd tandutinib Hs Inhibitor Inhibition 8.6 pKd 2.7 Kd pazopanib Hs Inhibitor Inhibition 8.6 pKd 2.8 Kd axitinib Hs Inhibitor Inhibition 8.5 pKd 3.2 Kd JNJ-28312141 Hs Inhibitor Inhibition 8.4 pKd 3.6 Kd motesanib Hs Inhibitor Inhibition 8.4 pKd 3.7 Kd quizartinib Hs Inhibitor Inhibition 8.3 pKd 4.8 Kd vatalanib Hs Inhibitor Inhibition 8.3 pKd 5.1 Kd AST-487 Hs Inhibitor Inhibition 8.3 pKd 5.4 Kd tamatinib Hs Inhibitor Inhibition 8.2 pKd 6.8 Kd dovitinib Hs Inhibitor Inhibition 8.1 pKd 7.5 Kd masitinib Hs Inhibitor Inhibition 8.1 pKd 8.1 Kd imatinib Hs Inhibitor Inhibition 7.9 pKd 13.0 Kd barasertib-hQPA Hs Inhibitor Inhibition 7.8 pKd 17.0 Kd staurosporine Hs Inhibitor Inhibition 7.7 pKd 19.0 Kd sorafenib Hs Inhibitor Inhibition 7.6 pKd 28.0 Kd nilotinib Hs Inhibitor Inhibition 7.5 pKd 29.0 Kd brivanib Hs Inhibitor Inhibition 7.4 pKd 36.0 Kd KW-2449 Hs Inhibitor Inhibition 7.3 pKd 53.0 Kd NVP-TAE684 Hs Inhibitor Inhibition 7.0 pKd 110.0 Kd fedratinib Hs Inhibitor Inhibition 6.9 pKd 130.0 Kd lestaurtinib Hs Inhibitor Inhibition 6.8 pKd 150.0 Kd doramapimod Hs Inhibitor Inhibition 6.8 pKd 170.0 Kd PLX-4720 Hs Inhibitor Inhibition 6.7 pKd 180.0 Kd CHIR-265 Hs Inhibitor Inhibition 6.7 pKd 200.0 Kd midostaurin Hs Inhibitor Inhibition 6.7 pKd 220.0 Kd tozasertib Hs Inhibitor Inhibition 6.6 pKd 240.0 Kd vandetanib Hs Inhibitor Inhibition 6.6 pKd 260.0 Kd PP-242 Hs Inhibitor Inhibition 6.4 pKd 360.0 Kd bosutinib Hs Inhibitor Inhibition 6.4 pKd 420.0 Kd erlotinib Hs Inhibitor Inhibition 5.8 pKd 1700.0 Kd MLN-8054 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd A-674563 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd SB203580 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd PI-103 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd ruboxistaurin Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd GSK690693 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd R547 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd SGX-523 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd gefitinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd TG-100-115 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd crizotinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd BMS-345541 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd BMS-387032 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd CI-1040 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd tofacitinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd BI-2536 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd selumetinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd alvocidib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd GDC-0879 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd pictilisib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd GSK-1838705A Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd GSK-461364A Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd GW-2580 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd neratinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd ruxolitinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd AT-7519 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd lapatinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd enzastaurin Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd MLN-120B Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd neflamapimod Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd afatinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd PHA-665752 Hs Inhibitor Inhibition 5.5 pKd 3200.0 Kd canertinib Hs Inhibitor Inhibition 5.1 pKd 7800.0 Kd
Target used in screen: KIT(A829P)
Ligand Sp. Type Action Value (-log10) Parameter Value (nM) Parameter staurosporine Hs Inhibitor Inhibition 9.2 pKd 0.6 Kd dasatinib Hs Inhibitor Inhibition 9.2 pKd 0.7 Kd foretinib Hs Inhibitor Inhibition 8.5 pKd 3.2 Kd tamatinib Hs Inhibitor Inhibition 8.5 pKd 3.5 Kd quizartinib Hs Inhibitor Inhibition 8.4 pKd 3.6 Kd AST-487 Hs Inhibitor Inhibition 8.4 pKd 4.4 Kd masitinib Hs Inhibitor Inhibition 7.9 pKd 12.0 Kd imatinib Hs Inhibitor Inhibition 7.8 pKd 15.0 Kd motesanib Hs Inhibitor Inhibition 7.8 pKd 15.0 Kd linifanib Hs Inhibitor Inhibition 7.8 pKd 17.0 Kd sorafenib Hs Inhibitor Inhibition 7.7 pKd 20.0 Kd tandutinib Hs Inhibitor Inhibition 7.6 pKd 23.0 Kd pazopanib Hs Inhibitor Inhibition 7.5 pKd 33.0 Kd vandetanib Hs Inhibitor Inhibition 7.5 pKd 34.0 Kd lestaurtinib Hs Inhibitor Inhibition 7.5 pKd 35.0 Kd Ki-20227 Hs Inhibitor Inhibition 7.4 pKd 38.0 Kd sunitinib Hs Inhibitor Inhibition 7.4 pKd 43.0 Kd midostaurin Hs Inhibitor Inhibition 7.4 pKd 43.0 Kd dovitinib Hs Inhibitor Inhibition 7.3 pKd 45.0 Kd nilotinib Hs Inhibitor Inhibition 7.3 pKd 46.0 Kd fedratinib Hs Inhibitor Inhibition 7.3 pKd 46.0 Kd SU-14813 Hs Inhibitor Inhibition 7.3 pKd 54.0 Kd PD-173955 Hs Inhibitor Inhibition 7.2 pKd 59.0 Kd JNJ-28312141 Hs Inhibitor Inhibition 7.2 pKd 60.0 Kd cediranib Hs Inhibitor Inhibition 7.0 pKd 98.0 Kd NVP-TAE684 Hs Inhibitor Inhibition 6.7 pKd 220.0 Kd bosutinib Hs Inhibitor Inhibition 6.6 pKd 270.0 Kd tozasertib Hs Inhibitor Inhibition 6.4 pKd 380.0 Kd barasertib-hQPA Hs Inhibitor Inhibition 6.2 pKd 600.0 Kd canertinib Hs Inhibitor Inhibition 6.2 pKd 700.0 Kd KW-2449 Hs Inhibitor Inhibition 6.1 pKd 860.0 Kd CHIR-265 Hs Inhibitor Inhibition 6.0 pKd 990.0 Kd doramapimod Hs Inhibitor Inhibition 5.8 pKd 1400.0 Kd PP-242 Hs Inhibitor Inhibition 5.8 pKd 1600.0 Kd GSK690693 Hs Inhibitor Inhibition 5.7 pKd 1800.0 Kd gefitinib Hs Inhibitor Inhibition 5.7 pKd 1800.0 Kd axitinib Hs Inhibitor Inhibition 5.7 pKd 1800.0 Kd MLN-120B Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd MLN-8054 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd AT-7519 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd PI-103 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd vatalanib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd A-674563 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd R547 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd SGX-523 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd crizotinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd brivanib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd BMS-345541 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd CI-1040 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd tofacitinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd afatinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd GDC-0879 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd pictilisib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd GSK-1838705A Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd GW-2580 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd neratinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd BI-2536 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd selumetinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd lapatinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd enzastaurin Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd SB203580 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd TG-100-115 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd erlotinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd neflamapimod Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd BMS-387032 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd ruboxistaurin Hs Inhibitor Inhibition 5.4 pKd 4100.0 Kd PHA-665752 Hs Inhibitor Inhibition 5.4 pKd 4300.0 Kd PLX-4720 Hs Inhibitor Inhibition 5.2 pKd 5800.0 Kd ruxolitinib Hs Inhibitor Inhibition 5.2 pKd 6300.0 Kd GSK-461364A Hs Inhibitor Inhibition 5.1 pKd 7200.0 Kd alvocidib Hs Inhibitor Inhibition 5.1 pKd 8800.0 Kd
Target used in screen: KIT(D816H)
Ligand Sp. Type Action Value (-log10) Parameter Value (nM) Parameter staurosporine Hs Inhibitor Inhibition 9.4 pKd 0.4 Kd dasatinib Hs Inhibitor Inhibition 8.8 pKd 1.6 Kd tamatinib Hs Inhibitor Inhibition 8.2 pKd 6.5 Kd lestaurtinib Hs Inhibitor Inhibition 8.0 pKd 11.0 Kd midostaurin Hs Inhibitor Inhibition 7.8 pKd 16.0 Kd foretinib Hs Inhibitor Inhibition 7.4 pKd 36.0 Kd JNJ-28312141 Hs Inhibitor Inhibition 7.3 pKd 48.0 Kd AST-487 Hs Inhibitor Inhibition 7.2 pKd 67.0 Kd sunitinib Hs Inhibitor Inhibition 7.0 pKd 110.0 Kd tandutinib Hs Inhibitor Inhibition 6.9 pKd 120.0 Kd NVP-TAE684 Hs Inhibitor Inhibition 6.8 pKd 140.0 Kd fedratinib Hs Inhibitor Inhibition 6.8 pKd 160.0 Kd dovitinib Hs Inhibitor Inhibition 6.8 pKd 170.0 Kd motesanib Hs Inhibitor Inhibition 6.7 pKd 180.0 Kd bosutinib Hs Inhibitor Inhibition 6.7 pKd 180.0 Kd KW-2449 Hs Inhibitor Inhibition 6.6 pKd 240.0 Kd SU-14813 Hs Inhibitor Inhibition 6.5 pKd 310.0 Kd quizartinib Hs Inhibitor Inhibition 6.5 pKd 320.0 Kd GSK690693 Hs Inhibitor Inhibition 6.4 pKd 360.0 Kd vandetanib Hs Inhibitor Inhibition 6.4 pKd 420.0 Kd sorafenib Hs Inhibitor Inhibition 6.4 pKd 430.0 Kd PD-173955 Hs Inhibitor Inhibition 6.3 pKd 470.0 Kd nilotinib Hs Inhibitor Inhibition 6.3 pKd 540.0 Kd imatinib Hs Inhibitor Inhibition 6.3 pKd 560.0 Kd canertinib Hs Inhibitor Inhibition 6.2 pKd 600.0 Kd cediranib Hs Inhibitor Inhibition 6.1 pKd 820.0 Kd pazopanib Hs Inhibitor Inhibition 6.0 pKd 1000.0 Kd linifanib Hs Inhibitor Inhibition 6.0 pKd 1100.0 Kd masitinib Hs Inhibitor Inhibition 5.8 pKd 1500.0 Kd ruboxistaurin Hs Inhibitor Inhibition 5.8 pKd 1500.0 Kd tozasertib Hs Inhibitor Inhibition 5.7 pKd 1900.0 Kd barasertib-hQPA Hs Inhibitor Inhibition 5.5 pKd 2900.0 Kd pictilisib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd GSK-1838705A Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd GSK-461364A Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd GW-2580 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd neratinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd BMS-345541 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd doramapimod Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd afatinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd lapatinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd enzastaurin Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd MLN-120B Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd BI-2536 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd MLN-8054 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd selumetinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd PI-103 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd AT-7519 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd PLX-4720 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd crizotinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd CI-1040 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd tofacitinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd brivanib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd BMS-387032 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd GDC-0879 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd vatalanib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd R547 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd SGX-523 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd SB203580 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd TG-100-115 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd erlotinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd neflamapimod Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd PP-242 Hs Inhibitor Inhibition 5.5 pKd 3500.0 Kd PHA-665752 Hs Inhibitor Inhibition 5.4 pKd 4000.0 Kd axitinib Hs Inhibitor Inhibition 5.4 pKd 4200.0 Kd A-674563 Hs Inhibitor Inhibition 5.4 pKd 4300.0 Kd gefitinib Hs Inhibitor Inhibition 5.3 pKd 5500.0 Kd ruxolitinib Hs Inhibitor Inhibition 5.2 pKd 6300.0 Kd Ki-20227 Hs Inhibitor Inhibition 5.2 pKd 7000.0 Kd CHIR-265 Hs Inhibitor Inhibition 5.1 pKd 8700.0 Kd alvocidib Hs Inhibitor Inhibition 5.1 pKd 9000.0 Kd
Target used in screen: KIT(D816V)
Ligand Sp. Type Action Value (-log10) Parameter Value (nM) Parameter staurosporine Hs Inhibitor Inhibition 9.2 pKd 0.6 Kd tamatinib Hs Inhibitor Inhibition 8.6 pKd 2.5 Kd dasatinib Hs Inhibitor Inhibition 8.6 pKd 2.6 Kd lestaurtinib Hs Inhibitor Inhibition 8.1 pKd 7.1 Kd midostaurin Hs Inhibitor Inhibition 8.1 pKd 7.7 Kd foretinib Hs Inhibitor Inhibition 8.0 pKd 9.6 Kd JNJ-28312141 Hs Inhibitor Inhibition 7.7 pKd 18.0 Kd NVP-TAE684 Hs Inhibitor Inhibition 7.6 pKd 26.0 Kd tandutinib Hs Inhibitor Inhibition 7.5 pKd 29.0 Kd PD-173955 Hs Inhibitor Inhibition 7.5 pKd 35.0 Kd bosutinib Hs Inhibitor Inhibition 7.1 pKd 73.0 Kd linifanib Hs Inhibitor Inhibition 7.1 pKd 81.0 Kd GSK690693 Hs Inhibitor Inhibition 6.9 pKd 130.0 Kd quizartinib Hs Inhibitor Inhibition 6.8 pKd 150.0 Kd fedratinib Hs Inhibitor Inhibition 6.8 pKd 160.0 Kd KW-2449 Hs Inhibitor Inhibition 6.8 pKd 160.0 Kd vandetanib Hs Inhibitor Inhibition 6.5 pKd 290.0 Kd tozasertib Hs Inhibitor Inhibition 6.5 pKd 290.0 Kd PP-242 Hs Inhibitor Inhibition 6.5 pKd 300.0 Kd sorafenib Hs Inhibitor Inhibition 6.5 pKd 310.0 Kd SU-14813 Hs Inhibitor Inhibition 6.5 pKd 340.0 Kd AST-487 Hs Inhibitor Inhibition 6.4 pKd 360.0 Kd sunitinib Hs Inhibitor Inhibition 6.4 pKd 380.0 Kd cediranib Hs Inhibitor Inhibition 6.4 pKd 390.0 Kd motesanib Hs Inhibitor Inhibition 6.4 pKd 410.0 Kd pazopanib Hs Inhibitor Inhibition 6.3 pKd 500.0 Kd Ki-20227 Hs Inhibitor Inhibition 6.2 pKd 580.0 Kd PHA-665752 Hs Inhibitor Inhibition 6.2 pKd 590.0 Kd ruboxistaurin Hs Inhibitor Inhibition 6.1 pKd 760.0 Kd nilotinib Hs Inhibitor Inhibition 6.1 pKd 770.0 Kd imatinib Hs Inhibitor Inhibition 6.0 pKd 980.0 Kd A-674563 Hs Inhibitor Inhibition 6.0 pKd 1000.0 Kd enzastaurin Hs Inhibitor Inhibition 6.0 pKd 1100.0 Kd axitinib Hs Inhibitor Inhibition 5.9 pKd 1300.0 Kd masitinib Hs Inhibitor Inhibition 5.9 pKd 1300.0 Kd dovitinib Hs Inhibitor Inhibition 5.8 pKd 1400.0 Kd GSK-461364A Hs Inhibitor Inhibition 5.8 pKd 1600.0 Kd erlotinib Hs Inhibitor Inhibition 5.8 pKd 1600.0 Kd GSK-1838705A Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd pictilisib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd GDC-0879 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd lapatinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd GW-2580 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd neratinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd R547 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd SGX-523 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd afatinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd BI-2536 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd selumetinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd AT-7519 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd TG-100-115 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd SB203580 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd neflamapimod Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd MLN-120B Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd tofacitinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd MLN-8054 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd CI-1040 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd PI-103 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd BMS-387032 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd BMS-345541 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd vatalanib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd doramapimod Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd PLX-4720 Hs Inhibitor Inhibition 5.5 pKd 3100.0 Kd crizotinib Hs Inhibitor Inhibition 5.4 pKd 3700.0 Kd canertinib Hs Inhibitor Inhibition 5.4 pKd 3900.0 Kd brivanib Hs Inhibitor Inhibition 5.4 pKd 4000.0 Kd gefitinib Hs Inhibitor Inhibition 5.4 pKd 4300.0 Kd alvocidib Hs Inhibitor Inhibition 5.3 pKd 4600.0 Kd barasertib-hQPA Hs Inhibitor Inhibition 5.3 pKd 4600.0 Kd CHIR-265 Hs Inhibitor Inhibition 5.2 pKd 6200.0 Kd ruxolitinib Hs Inhibitor Inhibition 5.2 pKd 7100.0 Kd
Target used in screen: KIT(L576P)
Ligand Sp. Type Action Value (-log10) Parameter Value (nM) Parameter SU-14813 Hs Inhibitor Inhibition 9.5 pKd 0.3 Kd cediranib Hs Inhibitor Inhibition 9.3 pKd 0.5 Kd dasatinib Hs Inhibitor Inhibition 9.2 pKd 0.6 Kd Ki-20227 Hs Inhibitor Inhibition 9.1 pKd 0.9 Kd sunitinib Hs Inhibitor Inhibition 8.9 pKd 1.3 Kd motesanib Hs Inhibitor Inhibition 8.9 pKd 1.3 Kd dovitinib Hs Inhibitor Inhibition 8.8 pKd 1.6 Kd axitinib Hs Inhibitor Inhibition 8.8 pKd 1.7 Kd pazopanib Hs Inhibitor Inhibition 8.7 pKd 1.8 Kd linifanib Hs Inhibitor Inhibition 8.7 pKd 1.9 Kd AST-487 Hs Inhibitor Inhibition 8.7 pKd 2.1 Kd JNJ-28312141 Hs Inhibitor Inhibition 8.6 pKd 2.3 Kd foretinib Hs Inhibitor Inhibition 8.6 pKd 2.7 Kd PD-173955 Hs Inhibitor Inhibition 8.4 pKd 3.7 Kd tamatinib Hs Inhibitor Inhibition 8.3 pKd 5.6 Kd tandutinib Hs Inhibitor Inhibition 8.2 pKd 6.0 Kd quizartinib Hs Inhibitor Inhibition 8.2 pKd 6.3 Kd masitinib Hs Inhibitor Inhibition 8.1 pKd 7.9 Kd imatinib Hs Inhibitor Inhibition 7.8 pKd 14.0 Kd KW-2449 Hs Inhibitor Inhibition 7.7 pKd 21.0 Kd staurosporine Hs Inhibitor Inhibition 7.7 pKd 22.0 Kd nilotinib Hs Inhibitor Inhibition 7.7 pKd 22.0 Kd sorafenib Hs Inhibitor Inhibition 7.6 pKd 25.0 Kd barasertib-hQPA Hs Inhibitor Inhibition 7.5 pKd 34.0 Kd lestaurtinib Hs Inhibitor Inhibition 7.4 pKd 40.0 Kd midostaurin Hs Inhibitor Inhibition 7.4 pKd 41.0 Kd NVP-TAE684 Hs Inhibitor Inhibition 7.3 pKd 49.0 Kd brivanib Hs Inhibitor Inhibition 7.3 pKd 54.0 Kd CHIR-265 Hs Inhibitor Inhibition 7.1 pKd 83.0 Kd vatalanib Hs Inhibitor Inhibition 7.0 pKd 110.0 Kd fedratinib Hs Inhibitor Inhibition 6.9 pKd 120.0 Kd vandetanib Hs Inhibitor Inhibition 6.8 pKd 140.0 Kd tozasertib Hs Inhibitor Inhibition 6.6 pKd 230.0 Kd doramapimod Hs Inhibitor Inhibition 6.6 pKd 260.0 Kd PP-242 Hs Inhibitor Inhibition 6.5 pKd 290.0 Kd PLX-4720 Hs Inhibitor Inhibition 6.4 pKd 400.0 Kd bosutinib Hs Inhibitor Inhibition 6.3 pKd 520.0 Kd PHA-665752 Hs Inhibitor Inhibition 5.9 pKd 1300.0 Kd GSK690693 Hs Inhibitor Inhibition 5.6 pKd 2600.0 Kd R547 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd SGX-523 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd gefitinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd crizotinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd afatinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd BMS-387032 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd CI-1040 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd tofacitinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd selumetinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd alvocidib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd GDC-0879 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd pictilisib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd GSK-1838705A Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd GSK-461364A Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd GW-2580 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd neratinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd ruxolitinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd AT-7519 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd lapatinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd MLN-120B Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd A-674563 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd MLN-8054 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd SB203580 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd PI-103 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd TG-100-115 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd neflamapimod Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd BI-2536 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd erlotinib Hs Inhibitor Inhibition 5.5 pKd 3500.0 Kd BMS-345541 Hs Inhibitor Inhibition 5.4 pKd 3900.0 Kd enzastaurin Hs Inhibitor Inhibition 5.3 pKd 5200.0 Kd canertinib Hs Inhibitor Inhibition 5.2 pKd 5700.0 Kd ruboxistaurin Hs Inhibitor Inhibition 5.1 pKd 7900.0 Kd
Target used in screen: KIT(V559D)
Ligand Sp. Type Action Value (-log10) Parameter Value (nM) Parameter cediranib Hs Inhibitor Inhibition 9.6 pKd 0.3 Kd sunitinib Hs Inhibitor Inhibition 9.4 pKd 0.4 Kd Ki-20227 Hs Inhibitor Inhibition 9.3 pKd 0.5 Kd axitinib Hs Inhibitor Inhibition 9.3 pKd 0.5 Kd SU-14813 Hs Inhibitor Inhibition 9.3 pKd 0.5 Kd dasatinib Hs Inhibitor Inhibition 9.2 pKd 0.7 Kd PD-173955 Hs Inhibitor Inhibition 8.8 pKd 1.6 Kd linifanib Hs Inhibitor Inhibition 8.8 pKd 1.7 Kd foretinib Hs Inhibitor Inhibition 8.7 pKd 2.1 Kd pazopanib Hs Inhibitor Inhibition 8.6 pKd 2.3 Kd motesanib Hs Inhibitor Inhibition 8.5 pKd 3.2 Kd tandutinib Hs Inhibitor Inhibition 8.4 pKd 3.8 Kd quizartinib Hs Inhibitor Inhibition 8.3 pKd 5.0 Kd AST-487 Hs Inhibitor Inhibition 8.3 pKd 5.0 Kd tamatinib Hs Inhibitor Inhibition 8.2 pKd 5.7 Kd masitinib Hs Inhibitor Inhibition 8.2 pKd 5.8 Kd dovitinib Hs Inhibitor Inhibition 8.1 pKd 7.2 Kd JNJ-28312141 Hs Inhibitor Inhibition 8.1 pKd 7.7 Kd staurosporine Hs Inhibitor Inhibition 7.8 pKd 15.0 Kd barasertib-hQPA Hs Inhibitor Inhibition 7.8 pKd 15.0 Kd imatinib Hs Inhibitor Inhibition 7.8 pKd 15.0 Kd sorafenib Hs Inhibitor Inhibition 7.8 pKd 16.0 Kd vatalanib Hs Inhibitor Inhibition 7.8 pKd 17.0 Kd KW-2449 Hs Inhibitor Inhibition 7.6 pKd 23.0 Kd brivanib Hs Inhibitor Inhibition 7.5 pKd 35.0 Kd PLX-4720 Hs Inhibitor Inhibition 7.4 pKd 38.0 Kd nilotinib Hs Inhibitor Inhibition 7.3 pKd 46.0 Kd fedratinib Hs Inhibitor Inhibition 7.2 pKd 58.0 Kd lestaurtinib Hs Inhibitor Inhibition 7.1 pKd 76.0 Kd NVP-TAE684 Hs Inhibitor Inhibition 7.1 pKd 81.0 Kd CHIR-265 Hs Inhibitor Inhibition 6.8 pKd 170.0 Kd vandetanib Hs Inhibitor Inhibition 6.7 pKd 180.0 Kd midostaurin Hs Inhibitor Inhibition 6.7 pKd 200.0 Kd doramapimod Hs Inhibitor Inhibition 6.6 pKd 230.0 Kd tozasertib Hs Inhibitor Inhibition 6.6 pKd 240.0 Kd PP-242 Hs Inhibitor Inhibition 6.6 pKd 260.0 Kd bosutinib Hs Inhibitor Inhibition 6.4 pKd 430.0 Kd PHA-665752 Hs Inhibitor Inhibition 5.6 pKd 2500.0 Kd tofacitinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd ruxolitinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd CI-1040 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd A-674563 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd lapatinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd enzastaurin Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd MLN-120B Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd SB203580 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd MLN-8054 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd ruboxistaurin Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd PI-103 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd BMS-387032 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd gefitinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd R547 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd SGX-523 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd BI-2536 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd alvocidib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd GDC-0879 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd pictilisib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd GSK-1838705A Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd GSK-461364A Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd GW-2580 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd neratinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd TG-100-115 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd afatinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd neflamapimod Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd AT-7519 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd crizotinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd selumetinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd erlotinib Hs Inhibitor Inhibition 5.5 pKd 3100.0 Kd BMS-345541 Hs Inhibitor Inhibition 5.2 pKd 5700.0 Kd GSK690693 Hs Inhibitor Inhibition 5.1 pKd 7300.0 Kd canertinib Hs Inhibitor Inhibition 5.1 pKd 7900.0 Kd
Target used in screen: KIT(V559D,T670I)
Ligand Sp. Type Action Value (-log10) Parameter Value (nM) Parameter sunitinib Hs Inhibitor Inhibition 9.6 pKd 0.3 Kd cediranib Hs Inhibitor Inhibition 9.5 pKd 0.3 Kd SU-14813 Hs Inhibitor Inhibition 9.3 pKd 0.6 Kd axitinib Hs Inhibitor Inhibition 8.9 pKd 1.4 Kd foretinib Hs Inhibitor Inhibition 8.6 pKd 2.4 Kd linifanib Hs Inhibitor Inhibition 8.4 pKd 3.8 Kd quizartinib Hs Inhibitor Inhibition 8.2 pKd 6.0 Kd pazopanib Hs Inhibitor Inhibition 8.2 pKd 6.5 Kd barasertib-hQPA Hs Inhibitor Inhibition 8.1 pKd 7.9 Kd staurosporine Hs Inhibitor Inhibition 8.0 pKd 9.5 Kd Ki-20227 Hs Inhibitor Inhibition 8.0 pKd 10.0 Kd tamatinib Hs Inhibitor Inhibition 8.0 pKd 11.0 Kd KW-2449 Hs Inhibitor Inhibition 7.9 pKd 12.0 Kd motesanib Hs Inhibitor Inhibition 7.9 pKd 13.0 Kd brivanib Hs Inhibitor Inhibition 7.8 pKd 17.0 Kd AST-487 Hs Inhibitor Inhibition 7.7 pKd 18.0 Kd sorafenib Hs Inhibitor Inhibition 7.7 pKd 18.0 Kd dovitinib Hs Inhibitor Inhibition 7.6 pKd 26.0 Kd JNJ-28312141 Hs Inhibitor Inhibition 7.4 pKd 39.0 Kd lestaurtinib Hs Inhibitor Inhibition 7.3 pKd 45.0 Kd NVP-TAE684 Hs Inhibitor Inhibition 6.9 pKd 130.0 Kd midostaurin Hs Inhibitor Inhibition 6.8 pKd 150.0 Kd nilotinib Hs Inhibitor Inhibition 6.8 pKd 150.0 Kd CHIR-265 Hs Inhibitor Inhibition 6.6 pKd 240.0 Kd doramapimod Hs Inhibitor Inhibition 6.6 pKd 260.0 Kd tozasertib Hs Inhibitor Inhibition 6.4 pKd 430.0 Kd crizotinib Hs Inhibitor Inhibition 6.1 pKd 800.0 Kd GSK690693 Hs Inhibitor Inhibition 6.0 pKd 1000.0 Kd tandutinib Hs Inhibitor Inhibition 6.0 pKd 1100.0 Kd erlotinib Hs Inhibitor Inhibition 5.9 pKd 1300.0 Kd fedratinib Hs Inhibitor Inhibition 5.8 pKd 1500.0 Kd PP-242 Hs Inhibitor Inhibition 5.8 pKd 1700.0 Kd canertinib Hs Inhibitor Inhibition 5.7 pKd 1900.0 Kd vandetanib Hs Inhibitor Inhibition 5.7 pKd 2000.0 Kd imatinib Hs Inhibitor Inhibition 5.6 pKd 2500.0 Kd masitinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd A-674563 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd lapatinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd enzastaurin Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd MLN-120B Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd MLN-8054 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd SB203580 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd BI-2536 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd PHA-665752 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd PI-103 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd PLX-4720 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd vatalanib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd R547 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd SGX-523 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd bosutinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd gefitinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd TG-100-115 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd neflamapimod Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd PD-173955 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd afatinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd BMS-345541 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd BMS-387032 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd selumetinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd CI-1040 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd tofacitinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd dasatinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd AT-7519 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd alvocidib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd GDC-0879 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd pictilisib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd GSK-1838705A Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd GSK-461364A Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd GW-2580 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd neratinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd ruxolitinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd ruboxistaurin Hs Inhibitor Inhibition 5.0 pKd 9800.0 Kd
Target used in screen: KIT(V559D,V654A)
Ligand Sp. Type Action Value (-log10) Parameter Value (nM) Parameter sunitinib Hs Inhibitor Inhibition 9.7 pKd 0.2 Kd SU-14813 Hs Inhibitor Inhibition 9.6 pKd 0.3 Kd cediranib Hs Inhibitor Inhibition 9.5 pKd 0.3 Kd dasatinib Hs Inhibitor Inhibition 8.6 pKd 2.7 Kd dovitinib Hs Inhibitor Inhibition 8.5 pKd 3.1 Kd Ki-20227 Hs Inhibitor Inhibition 8.5 pKd 3.2 Kd axitinib Hs Inhibitor Inhibition 8.5 pKd 3.5 Kd masitinib Hs Inhibitor Inhibition 8.3 pKd 4.7 Kd JNJ-28312141 Hs Inhibitor Inhibition 8.2 pKd 6.0 Kd foretinib Hs Inhibitor Inhibition 8.1 pKd 7.6 Kd brivanib Hs Inhibitor Inhibition 7.9 pKd 12.0 Kd linifanib Hs Inhibitor Inhibition 7.7 pKd 21.0 Kd motesanib Hs Inhibitor Inhibition 7.6 pKd 23.0 Kd tandutinib Hs Inhibitor Inhibition 7.6 pKd 26.0 Kd pazopanib Hs Inhibitor Inhibition 7.5 pKd 30.0 Kd quizartinib Hs Inhibitor Inhibition 7.4 pKd 36.0 Kd staurosporine Hs Inhibitor Inhibition 7.4 pKd 38.0 Kd PD-173955 Hs Inhibitor Inhibition 7.2 pKd 68.0 Kd KW-2449 Hs Inhibitor Inhibition 7.1 pKd 76.0 Kd imatinib Hs Inhibitor Inhibition 7.0 pKd 91.0 Kd AST-487 Hs Inhibitor Inhibition 7.0 pKd 100.0 Kd bosutinib Hs Inhibitor Inhibition 6.9 pKd 130.0 Kd vatalanib Hs Inhibitor Inhibition 6.7 pKd 210.0 Kd sorafenib Hs Inhibitor Inhibition 6.6 pKd 240.0 Kd nilotinib Hs Inhibitor Inhibition 6.6 pKd 260.0 Kd lestaurtinib Hs Inhibitor Inhibition 6.4 pKd 380.0 Kd tamatinib Hs Inhibitor Inhibition 6.4 pKd 410.0 Kd barasertib-hQPA Hs Inhibitor Inhibition 6.3 pKd 480.0 Kd vandetanib Hs Inhibitor Inhibition 6.3 pKd 560.0 Kd CHIR-265 Hs Inhibitor Inhibition 6.1 pKd 850.0 Kd NVP-TAE684 Hs Inhibitor Inhibition 5.9 pKd 1200.0 Kd midostaurin Hs Inhibitor Inhibition 5.8 pKd 1600.0 Kd tozasertib Hs Inhibitor Inhibition 5.6 pKd 2300.0 Kd doramapimod Hs Inhibitor Inhibition 5.6 pKd 2400.0 Kd R547 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd SGX-523 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd gefitinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd erlotinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd crizotinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd A-674563 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd AT-7519 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd SB203580 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd selumetinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd BI-2536 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd afatinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd BMS-345541 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd BMS-387032 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd CI-1040 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd tofacitinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd ruboxistaurin Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd alvocidib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd GDC-0879 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd pictilisib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd GSK-1838705A Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd GSK-461364A Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd GW-2580 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd neratinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd ruxolitinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd lapatinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd enzastaurin Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd MLN-120B Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd MLN-8054 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd PI-103 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd PP-242 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd TG-100-115 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd neflamapimod Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd fedratinib Hs Inhibitor Inhibition 5.5 pKd 3500.0 Kd GSK690693 Hs Inhibitor Inhibition 5.5 pKd 3500.0 Kd PLX-4720 Hs Inhibitor Inhibition 5.3 pKd 4800.0 Kd PHA-665752 Hs Inhibitor Inhibition 5.1 pKd 7200.0 Kd canertinib Hs Inhibitor Inhibition 5.1 pKd 7900.0 Kd
Target used in screen: KIT-autoinhibited
Ligand Sp. Type Action Value (-log10) Parameter Value (nM) Parameter dasatinib Hs Inhibitor Inhibition 8.9 pKd 1.2 Kd sunitinib Hs Inhibitor Inhibition 8.5 pKd 3.0 Kd Ki-20227 Hs Inhibitor Inhibition 7.3 pKd 54.0 Kd PD-173955 Hs Inhibitor Inhibition 7.0 pKd 91.0 Kd quizartinib Hs Inhibitor Inhibition 6.7 pKd 190.0 Kd staurosporine Hs Inhibitor Inhibition 6.3 pKd 460.0 Kd AST-487 Hs Inhibitor Inhibition 5.9 pKd 1200.0 Kd vatalanib Hs Inhibitor Inhibition 5.8 pKd 1500.0 Kd sorafenib Hs Inhibitor Inhibition 5.7 pKd 2200.0 Kd imatinib Hs Inhibitor Inhibition 5.3 pKd 4500.0 Kd lestaurtinib Hs Inhibitor Inhibition 5.1 pKd 7500.0 Kd bosutinib Hs Inhibitor Inhibition 5.1 pKd 9000.0 Kd tozasertib Hs Inhibitor Inhibition 4.8 pKd 14000.0 Kd nilotinib Hs Inhibitor Inhibition 4.8 pKd 15000.0 Kd midostaurin Hs Inhibitor Inhibition 4.5 pKd 30000.0 Kd